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PTH1R

gene
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Summary

PTH1R (parathyroid hormone 1 receptor, HGNC:9608) is a protein-coding gene on chromosome 3p21.31, encoding Parathyroid hormone/parathyroid hormone-related peptide receptor (Q03431). G-protein-coupled receptor for parathyroid hormone (PTH) and for parathyroid hormone-related peptide (PTHLH). It is haploinsufficient (ClinGen: sufficient evidence).

The protein encoded by this gene is a member of the G-protein coupled receptor family 2. This protein is a receptor for parathyroid hormone (PTH) and for parathyroid hormone-like hormone (PTHLH). The activity of this receptor is mediated by G proteins which activate adenylyl cyclase and also a phosphatidylinositol-calcium second messenger system. Defects in this receptor are known to be the cause of Jansen’s metaphyseal chondrodysplasia (JMC), chondrodysplasia Blomstrand type (BOCD), as well as enchodromatosis. Two transcript variants encoding the same protein have been found for this gene.

Source: NCBI Gene 5745 — RefSeq curated summary.

At a glance

  • Gene–disease (curated): primary failure of tooth eruption (Definitive, GenCC) — +3 more curated relationships
  • GWAS associations: 16
  • Clinical variants (ClinVar): 452 total — 20 pathogenic, 10 likely-pathogenic
  • Phenotypes (HPO): 179
  • Druggable target: yes — 3 molecules with ChEMBL bioactivity
  • Dosage sensitivity (ClinGen): haploinsufficiency sufficient evidence, triplosensitivity no evidence
  • MANE Select transcript: NM_000316

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:9608
Approved symbolPTH1R
Nameparathyroid hormone 1 receptor
Location3p21.31
Locus typegene with protein product
StatusApproved
Ensembl geneENSG00000160801
Ensembl biotypeprotein_coding
OMIM168468
Entrez5745

Gene structure

Transcript identifiers

Ensembl transcripts: 27 — 25 protein_coding, 1 nonsense_mediated_decay, 1 protein_coding_CDS_not_defined

ENST00000313049, ENST00000418619, ENST00000422115, ENST00000427125, ENST00000428220, ENST00000430002, ENST00000449590, ENST00000490109, ENST00000877354, ENST00000877355, ENST00000877356, ENST00000877357, ENST00000877358, ENST00000877359, ENST00000877360, ENST00000877361, ENST00000877362, ENST00000936357, ENST00000958962, ENST00000958963, ENST00000958964, ENST00000958965, ENST00000958966, ENST00000958967, ENST00000958968, ENST00000958969, ENST00000958970

RefSeq mRNA: 2 — MANE Select: NM_000316 NM_000316, NM_001184744

CCDS: CCDS2747

Canonical transcript exons

ENST00000449590 — 16 exons

ExonStartEnd
ENSE000010545644690102546901085
ENSE000010545754689866246898857
ENSE000012507684689930346899456
ENSE000016093614690327046903799
ENSE000016838374687772146877843
ENSE000017392954688351246883634
ENSE000017990574688106246881118
ENSE000034811494689390746894009
ENSE000035752164689785546897965
ENSE000035778564689837846898472
ENSE000035960774690141446901480
ENSE000035963984690252646902667
ENSE000036106484690176646901860
ENSE000036509914690274946902790
ENSE000036611644689807446898192
ENSE000036792984689573546895869

Expression profiles

Bgee: expression breadth ubiquitous, 219 present calls, max score 98.60.

FANTOM5 (CAGE): breadth broad, TPM avg 4.6348 / max 167.3129, expressed in 631 samples.

FANTOM5 promoters (13 alternative TSS)

Promoter IDTPM avgSamples expressed
365092.0364543
365071.4075331
365040.8863355
365050.090539
365030.073637
365080.059422
365020.020810
364990.01963
365100.01614
365060.01495

Top tissues by expression

285 total, by Bgee expression score (0-100, higher = more expressed):

TissueAnatomy IDExpression scoreQuality
adult mammalian kidneyUBERON:000008298.60gold quality
metanephros cortexUBERON:001053397.70gold quality
tibiaUBERON:000097997.68gold quality
right adrenal gland cortexUBERON:003582795.07gold quality
kidneyUBERON:000211394.66gold quality
adult organismUBERON:000702394.41gold quality
right lobe of liverUBERON:000111494.26gold quality
right adrenal glandUBERON:000123393.71gold quality
periodontal ligamentUBERON:000826693.55gold quality
kidney epitheliumUBERON:000481993.19gold quality
metanephric glomerulusUBERON:000473693.00gold quality
renal glomerulusUBERON:000007492.96gold quality
adrenal cortexUBERON:000123592.94gold quality
left adrenal gland cortexUBERON:003582592.66gold quality
metanephrosUBERON:000008192.62gold quality
left adrenal glandUBERON:000123492.19gold quality
cortex of kidneyUBERON:000122591.72gold quality
right lungUBERON:000216791.31gold quality
nephron tubuleUBERON:000123191.18gold quality
apex of heartUBERON:000209891.02gold quality
adrenal glandUBERON:000236990.51gold quality
omental fat padUBERON:001041490.14gold quality
peritoneumUBERON:000235890.08gold quality
renal medullaUBERON:000036289.92gold quality
spleenUBERON:000210689.65gold quality
adipose tissue of abdominal regionUBERON:000780889.34gold quality
endocervixUBERON:000045889.28gold quality
mucosa of stomachUBERON:000119988.32gold quality
primordial germ cell in gonadCL:0000670 ∩ UBERON:000099188.10gold quality
left coronary arteryUBERON:000162687.91gold quality

Single-cell (SCXA)

Detected in 6 experiment(s), a significant marker in 6.

ExperimentMarker?Max mean expression
E-GEOD-131882yes2462.00
E-GEOD-130473yes700.89
E-CURD-119yes63.93
E-CURD-112yes16.11
E-HCAD-10yes15.44
E-ANND-3yes9.51

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): FOS, MAZ, MEF2C, SLC24A3, SP1, VDR, XBP1

miRNA regulators (miRDB)

7 targeting PTH1R, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-4481100.0066.421669
HSA-MIR-4745-5P99.9865.951028
HSA-MIR-431999.7669.832586
HSA-MIR-4446-5P99.7269.192544
HSA-MIR-3059-5P99.7069.932491
HSA-MIR-133A-3P99.2771.531270
HSA-MIR-133B99.2771.531270

Functional genomics

ClinGen dosage: haploinsufficiency 3 (sufficient evidence), triplosensitivity 0 (no evidence). ClinGen Gene Dosage Map

Literature-anchored findings (GeneRIF, showing 40)

  • different domains of PTHR implicated in agonist-dependent receptor internalization; the receptor’s core (Asn-289 and Lys-382) appears to regulate internalization of the receptor/beta-arrestin complex toward early endocytic endosomes during endocytosis. (PMID:11726668)
  • mutant expression in enchondromatosis (PMID:11850620)
  • Na(+)/H(+ ) exchanger regulatory factor 2 directs parathyroid hormone 1 receptor signalling (PMID:12075354)
  • These results show how specific interactions between PTH1Rc and its ligands may stabilize distinct conformational states, representing either the active G protein-coupled or a desensitized beta-arrestin-coupled receptor state. (PMID:12107160)
  • vascular sites of expression of PTHrP and its cognate receptor in the rheumatoid synovium and/or in cultured rheumatoid synovial endothelial cells (PMID:12359237)
  • expression is preserved in the growth plate of human fetuses affected with fibroblast growth factor receptor type 3 activating mutations (PMID:12368206)
  • The juxtamembrane region of the PTH-1 receptor interacts with parathyroid hormone (PTH) via a mechanism that involves the N-terminal portion of the ligand and residues 15-20, particularly residue 19, of PTH. (PMID:12403624)
  • The parathyroid hormone-related protein receptor is expressed in breast cancer bone metastases and promotes autocrine proliferation in breast carcinoma cells. (PMID:12592371)
  • collagenases can be a downstream effector of PTH/PTHrP receptor action in trabecular bone, but not in periosteum. (PMID:12933685)
  • Binds to a specific sites of PTH-related protein. (PMID:12947048)
  • PTHrP is an essential growth factor for clear cell renal carcinoma and is a novel target for the von Hippel-Lindau tumor suppressor protein. (PMID:14729622)
  • factors present in uremia hemodialysis ultrafiltrate decrease PTH-stimulated cAMP generation by a mechanism that involves a decrease in the levels of PTH1R mRNA levels. (PMID:14871409)
  • The PTH1R C terminus contains regulatory sequences that are involved in, but not required for, PTH1R internalization. The results demonstrate that receptor activation and internalization can be selectively dissociated. (PMID:15016722)
  • haplotype frequencies and linkage disequilibrium (LD) analysis of four different polymorphisms at the PTHR1 locus (PMID:15294324)
  • results indicate that the PTHR1 gene is not the culprit for enchondromatosis (PMID:15523647)
  • GSK3 and PKB/Akt have roles in the integrin-mediated regulation of PTHrP, IL-6 and IL-8 in pancreatic cancer (PMID:15609321)
  • PTH1R trafficking and G(q) (but not G(s)) signaling independently contribute to ERK1/2 activation, predominantly via transactivation of the epidermal growth factor receptor. (PMID:15611080)
  • PTH1R cytoplasmic tail interacts with calmodulin in a calcium-dependent manner via the basic 1-5-8-14 motif (PMID:15670850)
  • Cytoskeletal protein 4.1G facilitates the cell-surface localization of PTHR through its interaction with the C-terminus of the receptor, resulting in the potentiation of PTHR-mediated signal transduction. (PMID:16029167)
  • Manumycin inhibits cell proliferation and decreases PTHrP levels in anaplastic thyroid cancer cells in vitro and in vivo and decreases the PTHrP level in the nucleus. (PMID:16213899)
  • the conformational change that switches the receptor into its active state proceeds in a sequential manner, with the first rapid binding step event preceding receptor activation by PTH(1-34) (PMID:16236727)
  • Review. The multiple roles of PTHR1 in cell differentiation & proliferation in many organs, especially endochondral bone, and chondrodysplasias due to its mutation are reviewed. (PMID:16274647)
  • beta-arrestin and G proteins activate parathyroid hormone receptor-stimulated ERK1/2 pathways (PMID:16492667)
  • CCN2 was critically involved in osteolytic metastasis and was induced by PKA- and PKC-dependent activation of ERK1/2 signaling by PTHrP. (PMID:16813525)
  • PTHrP, TGF-beta1, and VEGF expression was significantly altered and indicated degenerative changes in Kashin-Beck disease cartilage (PMID:16816927)
  • data delineate multiple PTH1R structural determinants for ERK1/2 activation and identify unique mechanism involving proline-rich motifs in receptor C terminus for reciprocal scaffolding of c-Src and beta-arrestin2 with class II G-protein-coupled receptor (PMID:17038311)
  • PTHrP induces HHM and concurrent cachectic syndromes by mechanisms other than directly modulating the leptin or hypothalamic feeding-regulated peptides (PMID:17200368)
  • cysteine at position 217 in plays a critical role in translocation to the cell surface and biological function of PTHR1 (PMID:17227205)
  • Increased cell survival, migration, invasion, and Akt expression were studied in PTHR-overexpressing LoVo colon cancer cell lines. (PMID:17276526)
  • Coexpression of Etsl and CBP induced a synergistic activation of the parathyroid hormone-related protein P3 promoter only in the tumorigenic cell line. (PMID:17321669)
  • Modulation of cell adhesion is a normal physiological action of parathyroid hormone, mediated by increasing integrin gene transcription. (PMID:17406357)
  • PTHR1 over-expression may promote osteosarcoma progression by conferring a more aggressive phenotype, and forming a more favorable microenvironment (PMID:17410535)
  • constitutive activation of PTH/PTHrP receptor signaling in osteoblastic cells suppresses unloading-induced bone loss specifically through the regulation of osteoclastic activity. (PMID:17500070)
  • A microtubule-facilitated nuclear import pathway for PTHR is descibed. (PMID:17511743)
  • Results conclude that PTH and PTHrP bind similarly to the G protein-coupled PTHR conformation, PTH has a greater capacity to bind to the G protein-uncoupled conformation. (PMID:17872377)
  • that NHERF1 inhibits endocytosis without affecting PTH1R recycling (PMID:17884816)
  • PTHR1 polymorphisms influence bone density variation through effects on the growing skeleton. (PMID:17885720)
  • findings suggest that one of the pathways via which 1,25(OH)(2)D(3) exerts its anti-proliferative effects is through down-regulation of PTHrP expression (PMID:17904173)
  • These data indicate that PTHrP contributes to the malignancy of oral cancers downstream of EGFR signaling, and may thus provide a therapeutic target for oral cancer. (PMID:18261460)
  • 6 SNPs in the PTH gene and 3 SNPs each in the PTHLH, PTHR1 and PTHR2 genes were investigated in relation to bone mineral density (PMID:18280230)

Cross-species orthologs

3 orthologs

OrganismSymbolGene ID
danio_reriopth1rENSDARG00000020957
mus_musculusPth1rENSMUSG00000032492
rattus_norvegicusPth1rENSRNOG00000020948

Paralogs (42): CALCR (ENSG00000004948), GIPR (ENSG00000010310), ADGRA2 (ENSG00000020181), CALCRL (ENSG00000064989), GLP2R (ENSG00000065325), ADGRF5 (ENSG00000069122), ADGRL1 (ENSG00000072071), ADCYAP1R1 (ENSG00000078549), SCTR (ENSG00000080293), VIPR2 (ENSG00000106018), CRHR2 (ENSG00000106113), GHRHR (ENSG00000106128), ADGRD1 (ENSG00000111452), GLP1R (ENSG00000112164), ADGRG6 (ENSG00000112414), VIPR1 (ENSG00000114812), ADGRL2 (ENSG00000117114), CRHR1 (ENSG00000120088), ADGRB2 (ENSG00000121753), ADGRE5 (ENSG00000123146), ADGRE2 (ENSG00000127507), ADGRE3 (ENSG00000131355), ADGRB3 (ENSG00000135298), PTH2R (ENSG00000144407), ADGRG7 (ENSG00000144820), ADGRL3 (ENSG00000150471), ADGRA3 (ENSG00000152990), ADGRF1 (ENSG00000153292), ADGRF4 (ENSG00000153294), ADGRG4 (ENSG00000156920), ADGRG5 (ENSG00000159618), ADGRL4 (ENSG00000162618), EVA1C (ENSG00000166979), ADGRF3 (ENSG00000173567), ADGRG2 (ENSG00000173698), ADGRE1 (ENSG00000174837), ADGRD2 (ENSG00000180264), ADGRB1 (ENSG00000181790), ADGRG3 (ENSG00000182885), ADGRA1 (ENSG00000197177)

Protein

Protein identifiers

Parathyroid hormone/parathyroid hormone-related peptide receptor — Q03431 (reviewed: Q03431)

Alternative names: PTH/PTHrP type I receptor, Parathyroid hormone 1 receptor

All UniProt accessions (4): Q03431, E7EWE7, F2Z314, H7C0Q3

UniProt curated annotations — full annotation on UniProt →

Function. G-protein-coupled receptor for parathyroid hormone (PTH) and for parathyroid hormone-related peptide (PTHLH). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors, such as adenylate cyclase (cAMP). PTH1R is coupled to G(s) G alpha proteins and mediates activation of adenylate cyclase activity. PTHLH dissociates from PTH1R more rapidly than PTH; as consequence, the cAMP response induced by PTHLH decays faster than the response induced by PTH.

Subunit / interactions. Homodimer in the absence of bound ligand. Peptide hormone binding leads to dissociation of the homodimer.

Subcellular location. Cell membrane.

Tissue specificity. Expressed in most tissues. Most abundant in kidney, bone and liver.

Post-translational modifications. N-glycosylated.

Disease relevance. Metaphyseal chondrodysplasia, Jansen type (MCDJ) [MIM:156400] A rare autosomal dominant disorder characterized by a short-limbed dwarfism associated with hypercalcemia and normal or low serum concentrations of the two parathyroid hormones. The disease is caused by variants affecting the gene represented in this entry. Chondrodysplasia Blomstrand type (BOCD) [MIM:215045] Severe skeletal dysplasia. The disease is caused by variants affecting the gene represented in this entry. Eiken syndrome (EKNS) [MIM:600002] An autosomal recessive skeletal dysplasia characterized by severely retarded ossification, principally of the epiphyses, pelvis, hands and feet, as well as by abnormal modeling of the bones in hands and feet, abnormal persistence of cartilage in the pelvis and mild growth retardation. The disease is caused by variants affecting the gene represented in this entry. Primary failure of tooth eruption (PFE) [MIM:125350] Rare condition that has high penetrance and variable expressivity and in which tooth retention occurs without evidence of any obvious mechanical interference. Instead, malfunction of the eruptive mechanism itself appears to cause nonankylosed permanent teeth to fail to erupt, although the eruption pathway has been cleared by bone resorption. The disease is caused by variants affecting the gene represented in this entry.

Similarity. Belongs to the G-protein coupled receptor 2 family.

RefSeq proteins (2): NP_000307, NP_001171673 (=MANE)

Domains & families (InterPro)

IDNameType
IPR000832GPCR_2_secretin-likeFamily
IPR001879GPCR_2_extracellular_domDomain
IPR002170GPCR_2_parathyroid_rcptFamily
IPR017981GPCR_2-like_7TMDomain
IPR017983GPCR_2_secretin-like_CSConserved_site
IPR036445GPCR_2_extracell_dom_sfHomologous_superfamily
IPR050332GPCR_2Family

Pfam: PF00002, PF02793

UniProt features (69 total): helix 14, strand 9, topological domain 8, transmembrane region 7, sequence variant 6, mutagenesis site 5, glycosylation site 4, turn 4, disulfide bond 3, region of interest 2, sequence conflict 2, signal peptide 1, chain 1, short sequence motif 1, compositionally biased region 1, modified residue 1

Structure

Experimental structures (PDB)

48 structures, top 30 by resolution.

PDBMethodResolution (Å)
5EMBX-RAY DIFFRACTION0.85
4Z8JX-RAY DIFFRACTION0.95
7UZOX-RAY DIFFRACTION1.3
3H3GX-RAY DIFFRACTION1.94
3C4MX-RAY DIFFRACTION1.95
8D51X-RAY DIFFRACTION2
8D52X-RAY DIFFRACTION2.02
7UZPX-RAY DIFFRACTION2.29
8BIAX-RAY DIFFRACTION2.4
6FJ3X-RAY DIFFRACTION2.5
8FLQELECTRON MICROSCOPY2.55
8JR9ELECTRON MICROSCOPY2.57
8YG4ELECTRON MICROSCOPY2.59
8BJ0X-RAY DIFFRACTION2.6
8HA0ELECTRON MICROSCOPY2.62
8YFOELECTRON MICROSCOPY2.71
8FLUELECTRON MICROSCOPY2.76
7VVLELECTRON MICROSCOPY2.8
7Y36ELECTRON MICROSCOPY2.8
9JR2ELECTRON MICROSCOPY2.8
9JR3ELECTRON MICROSCOPY2.8
25NXELECTRON MICROSCOPY2.86
7Y35ELECTRON MICROSCOPY2.9
8GW8ELECTRON MICROSCOPY2.9
8FLRELECTRON MICROSCOPY2.94
6NBFELECTRON MICROSCOPY3
9LZ2ELECTRON MICROSCOPY3
8FLTELECTRON MICROSCOPY3.03
9LXRELECTRON MICROSCOPY3.07
8FLSELECTRON MICROSCOPY3.09

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q03431-F172.290.37

Antibody-complex structures (SAbDab): 27 — 6NBF, 6NBH, 6NBI, 7VVJ, 7VVK, 7VVL, 7VVM, 7VVN, 7VVO, 7Y35, 7Y36, 8FLQ, 8FLR, 8FLS, 8FLT, 8FLU, 8GW8, 8HA0, 8HAF, 8HAO, 8JR9, 8YFO, 8YG4, 9B5Y, 9JR2 (+2 more)

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Post-translational modifications (1): 551

Disulfide bonds (3): 48–117, 108–148, 131–170

Glycosylation sites (4): 151, 161, 166, 176

Mutagenesis-validated functional residues (5):

PositionPhenotype
35slightly increased parathyroid hormone (pth) efficiency and decreased potency for parathyroid hormone-related peptide (p
135abolishes hormone binding and homodimerization.
137abolishes parathyroid hormone (pth) and parathyroid hormone-related peptide (pthlh) hormone-binding. no effect on homodi
195decreased potencies of parathyroid hormone (pth) and parathyroid hormone-related peptide (pthlh).
233decreased potencies of parathyroid hormone (pth) and parathyroid hormone-related peptide (pthlh).

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

IDPathway
R-HSA-373080Class B/2 (Secretin family receptors)
R-HSA-418555G alpha (s) signalling events

MSigDB gene sets: 587 (showing top): GOBP_EMBRYO_DEVELOPMENT_ENDING_IN_BIRTH_OR_EGG_HATCHING, GRUETZMANN_PANCREATIC_CANCER_DN, GOBP_CARTILAGE_DEVELOPMENT, GOBP_SKELETAL_SYSTEM_DEVELOPMENT, ENK_UV_RESPONSE_KERATINOCYTE_UP, GCANCTGNY_MYOD_Q6, MODULE_64, GOBP_INOSITOL_PHOSPHATE_METABOLIC_PROCESS, KAAB_HEART_ATRIUM_VS_VENTRICLE_UP, GOBP_POLYOL_METABOLIC_PROCESS, GOBP_OSTEOBLAST_DIFFERENTIATION, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, FOXO4_01, LHX3_01, GOBP_POSITIVE_REGULATION_OF_ALCOHOL_BIOSYNTHETIC_PROCESS

GO Biological Process (20): skeletal system development (GO:0001501), in utero embryonic development (GO:0001701), chondrocyte differentiation (GO:0002062), osteoblast development (GO:0002076), intracellular calcium ion homeostasis (GO:0006874), cell surface receptor signaling pathway (GO:0007166), G protein-coupled receptor signaling pathway (GO:0007186), G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger (GO:0007187), adenylate cyclase-modulating G protein-coupled receptor signaling pathway (GO:0007188), adenylate cyclase-activating G protein-coupled receptor signaling pathway (GO:0007189), phospholipase C-activating G protein-coupled receptor signaling pathway (GO:0007200), cell population proliferation (GO:0008283), positive regulation of cell population proliferation (GO:0008284), negative regulation of cell population proliferation (GO:0008285), bone mineralization (GO:0030282), bone resorption (GO:0045453), cell maturation (GO:0048469), positive regulation of inositol phosphate biosynthetic process (GO:0060732), ossification (GO:0001503), signal transduction (GO:0007165)

GO Molecular Function (7): G protein-coupled receptor activity (GO:0004930), parathyroid hormone receptor activity (GO:0004991), G protein-coupled peptide receptor activity (GO:0008528), peptide hormone binding (GO:0017046), protein homodimerization activity (GO:0042803), transmembrane signaling receptor activity (GO:0004888), protein binding (GO:0005515)

GO Cellular Component (9): nucleus (GO:0005634), nucleolus (GO:0005730), cytoplasm (GO:0005737), cytosol (GO:0005829), plasma membrane (GO:0005886), basolateral plasma membrane (GO:0016323), apical plasma membrane (GO:0016324), signaling receptor complex (GO:0043235), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-2 pathways:

CategoryPathways
GPCR ligand binding1
GPCR downstream signalling1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
G protein-coupled receptor signaling pathway4
G protein-coupled receptor activity3
cellular anatomical structure3
cell development2
signal transduction2
cellular process2
cell population proliferation2
regulation of cell population proliferation2
plasma membrane region2
system development1
chordate embryonic development1
cell differentiation1
cartilage development1
osteoblast differentiation1
intracellular monoatomic cation homeostasis1
calcium ion homeostasis1
adenylate cyclase activity1
adenylate cyclase-modulating G protein-coupled receptor signaling pathway1
adenylate cyclase activator activity1
phospholipase C activator activity1
positive regulation of cellular process1
negative regulation of cellular process1
ossification1
biomineral tissue development1
tissue homeostasis1
bone remodeling1
cellular developmental process1
anatomical structure maturation1
positive regulation of phosphorus metabolic process1
regulation of inositol phosphate biosynthetic process1
inositol phosphate biosynthetic process1
positive regulation of carbohydrate metabolic process1
positive regulation of alcohol biosynthetic process1
multicellular organismal process1
cell communication1
signaling1
regulation of cellular process1
cellular response to stimulus1
transmembrane signaling receptor activity1
peptide receptor activity1

Protein interactions and networks

STRING

1344 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
PTH1RPTHP01270999
PTH1RPTHLHP12272999
PTH1RLRP6O75581983
PTH1RSOSTQ9BQB4851
PTH1RNHERF1O14745850
PTH1RARRB1P49407816
PTH1RARRB2P32121814
PTH1RPTH2Q96A98781
PTH1RGHRHP01286764
PTH1RIHHQ14623740
PTH1RSTX16O14662685
PTH1RGNASQ5JWF2683
PTH1RNHERF2Q15599659
PTH1RCALM1P02593634
PTH1RLRP5O75197627

IntAct

167 interactions, top by confidence:

ABTypeScore
PTH1RPTHpsi-mi:“MI:0915”(physical association)0.610
PTH1RPTHpsi-mi:“MI:0407”(direct interaction)0.610
PTH1RPTHLHpsi-mi:“MI:0407”(direct interaction)0.610
PTH1RGUCD1psi-mi:“MI:0915”(physical association)0.560
PTH1RSMARCC1psi-mi:“MI:0915”(physical association)0.560
PTH1RMKRN3psi-mi:“MI:0915”(physical association)0.560
PTH1Rpsi-mi:“MI:0915”(physical association)0.560
HOXA1PTH1Rpsi-mi:“MI:0915”(physical association)0.560
GPANK1PTH1Rpsi-mi:“MI:0915”(physical association)0.560
STK16PTH1Rpsi-mi:“MI:0915”(physical association)0.560
PTH1RTEKT4psi-mi:“MI:0915”(physical association)0.560
CTNNB1PTH1Rpsi-mi:“MI:0915”(physical association)0.500
PTH1RCTNNB1psi-mi:“MI:0915”(physical association)0.500
PTH1RCTNNB1psi-mi:“MI:2364”(proximity)0.500
PTH1RCTNNB1psi-mi:“MI:0403”(colocalization)0.500
YWHAHPTH1Rpsi-mi:“MI:0407”(direct interaction)0.490
YWHAHPTH1Rpsi-mi:“MI:0403”(colocalization)0.490
CALM1PTH1Rpsi-mi:“MI:0403”(colocalization)0.460
PTH1RCALM1psi-mi:“MI:0915”(physical association)0.460
PTH1RMAST2psi-mi:“MI:0407”(direct interaction)0.440
PTH1RSNX27psi-mi:“MI:0407”(direct interaction)0.440
PTH1RPDZK1psi-mi:“MI:0407”(direct interaction)0.440
PTH1RNHERF2psi-mi:“MI:0407”(direct interaction)0.440
PTH1RMAST1psi-mi:“MI:0407”(direct interaction)0.440

BioGRID (122): DNAJC17 (Affinity Capture-MS), MBOAT7 (Affinity Capture-MS), CUX1 (Affinity Capture-MS), ATP12A (Affinity Capture-MS), PIGO (Affinity Capture-MS), SLC12A9 (Affinity Capture-MS), TMX2 (Affinity Capture-MS), SREBF2 (Affinity Capture-MS), SLC4A2 (Affinity Capture-MS), RETSAT (Affinity Capture-MS), AGPAT3 (Affinity Capture-MS), SPPL2B (Affinity Capture-MS), SLC12A7 (Affinity Capture-MS), SLC12A4 (Affinity Capture-MS), SLC30A1 (Affinity Capture-MS)

ESM2 similar proteins: A0A2Z2U4G9, O35659, O46502, O95838, P23811, P25107, P25117, P25961, P30082, P30083, P30988, P32082, P32214, P32215, P32241, P32301, P34999, P35000, P41587, P41588, P41593, P43218, P43219, P43220, P47871, P47872, P48546, P49190, P50133, P51839, P70555, P79222, P97751, Q02643, Q02644, Q03431, Q0P543, Q1LZF7, Q28992, Q29627

Diamond homologs: A0A2Z2U4G9, A6QP74, O35659, O42602, O42603, O46502, O62772, O95838, P23811, P25107, P25117, P25961, P30082, P30083, P32082, P32215, P32241, P32301, P34998, P34999, P35000, P35347, P35353, P41586, P41587, P41588, P41593, P43218, P43219, P43220, P47866, P47871, P47872, P48546, P48960, P49190, P50133, P70205, P70555, P97751

SIGNOR signaling

12 interactions.

AEffectBMechanism
PTHup-regulatesPTH1Rbinding
PTH1Rup-regulatesLRP6binding
“Parathyroid hormone-related peptide (1-36)”“up-regulates activity”PTH1R“chemical activation”
PTHLH“up-regulates activity”PTH1Rbinding
PTH1R“up-regulates activity”GNAQbinding
PTH1R“up-regulates activity”GNASbinding
PTH1R“down-regulates quantity”SOST
PTH1R“down-regulates quantity”DKK1
PTH1R“up-regulates quantity”CYP27B1
PTH1R“up-regulates quantity”CYP24A1
PTH1R“down-regulates quantity”SLC34A1
PTH1R“down-regulates quantity”SLC34A3

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 96 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

PathwayPartnersFoldFDR
Ras activation upon Ca2+ influx through NMDA receptor657.1×6e-08
Unblocking of NMDA receptors, glutamate binding and activation654.4×6e-08
Negative regulation of NMDA receptor-mediated neuronal transmission654.4×6e-08
Long-term potentiation647.6×1e-07
Assembly and cell surface presentation of NMDA receptors1042.3×4e-12
Dopamine Neurotransmitter Release Cycle541.4×5e-06
Neurexins and neuroligins1136.1×2e-12
Protein-protein interactions at synapses731.0×1e-07

GO biological processes:

GO termPartnersFoldFDR
establishment or maintenance of epithelial cell apical/basal polarity1170.2×1e-15
protein localization to synapse650.5×2e-07
receptor clustering748.0×3e-08
regulation of postsynaptic membrane neurotransmitter receptor levels738.1×1e-07
cell-cell adhesion1112.3×2e-07
protein-containing complex assembly911.3×9e-06
chemical synaptic transmission86.8×1e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

452 variants total. Per-class counts are floors (≥ shown; pagination cap):

ClassificationCount (floor)
Pathogenic20
Likely pathogenic10
Uncertain significance240
Likely benign108
Benign17

Top pathogenic / likely-pathogenic (30)

Variant IDHGVSClassification
1030731NM_000316.3(PTH1R):c.1373T>A (p.Ile458Lys)Pathogenic
13742NM_000316.3(PTH1R):c.668A>G (p.His223Arg)Pathogenic
13743NM_000316.3(PTH1R):c.1228A>C (p.Thr410Pro)Pathogenic
13744NM_000316.3(PTH1R):c.1148G>A (p.Arg383Gln)Pathogenic
13746NM_000316.3(PTH1R):c.1093del (p.Val365fs)Pathogenic
13747NM_000316.3(PTH1R):c.1373T>G (p.Ile458Arg)Pathogenic
13748NM_000316.3(PTH1R):c.1229C>G (p.Thr410Arg)Pathogenic
13749NM_000316.3(PTH1R):c.1453C>T (p.Arg485Ter)Pathogenic
13750NM_000316.3(PTH1R):c.310C>T (p.Arg104Ter)Pathogenic
13751NM_000316.3(PTH1R):c.1049+29C>TPathogenic
13752NM_000316.3(PTH1R):c.1050-3C>GPathogenic
13753NM_000316.3(PTH1R):c.543+1G>APathogenic
13754NM_000316.3(PTH1R):c.463G>T (p.Glu155Ter)Pathogenic
1686109NM_000316.3(PTH1R):c.639-2A>GPathogenic
1708330NM_000316.3(PTH1R):c.1201C>T (p.Gln401Ter)Pathogenic
3720496NM_000316.3(PTH1R):c.996dup (p.Ala333fs)Pathogenic
4075759NM_000316.3(PTH1R):c.1353+1G>TPathogenic
4075760NM_000316.3(PTH1R):c.665T>G (p.Ile222Ser)Pathogenic
4075801NM_000316.3(PTH1R):c.685T>C (p.Ser229Pro)Pathogenic
4819124NM_000316.3(PTH1R):c.1234del (p.Val412fs)Pathogenic
1301904NM_000316.3(PTH1R):c.723C>G (p.Asp241Glu)Likely pathogenic
1709439NM_000316.3(PTH1R):c.915C>G (p.Tyr305Ter)Likely pathogenic
2500163NM_000316.3(PTH1R):c.1325_1336del (p.His442_Met445del)Likely pathogenic
3338640NM_000316.3(PTH1R):c.1405G>A (p.Glu469Lys)Likely pathogenic
3393185NM_000316.3(PTH1R):c.989-2A>GLikely pathogenic
3589193NM_000316.3(PTH1R):c.75+1delLikely pathogenic
3589206NM_000316.3(PTH1R):c.735C>G (p.Tyr245Ter)Likely pathogenic
3589209NM_000316.3(PTH1R):c.892T>G (p.Trp298Gly)Likely pathogenic
4762291NM_000316.3(PTH1R):c.1212-2A>TLikely pathogenic
592121NM_000316.3(PTH1R):c.611T>A (p.Val204Glu)Likely pathogenic

SpliceAI

3026 predictions. Top by Δscore:

VariantEffectΔscore
3:46895723:T:TAacceptor_gain1.0000
3:46895733:A:AGacceptor_gain1.0000
3:46895734:G:GGacceptor_gain1.0000
3:46895734:GCCA:Gacceptor_gain1.0000
3:46898225:GA:Gdonor_gain1.0000
3:46898714:A:AGacceptor_gain1.0000
3:46898714:AT:Aacceptor_gain1.0000
3:46898714:ATGCT:Aacceptor_gain1.0000
3:46898715:T:Gacceptor_gain1.0000
3:46898715:T:TAacceptor_gain1.0000
3:46898718:T:Aacceptor_gain1.0000
3:46898853:GC:Gdonor_gain1.0000
3:46898853:GCTAC:Gdonor_gain1.0000
3:46898854:C:Gdonor_gain1.0000
3:46898854:CTAC:Cdonor_gain1.0000
3:46898855:TAC:Tdonor_gain1.0000
3:46898855:TACGT:Tdonor_loss1.0000
3:46898856:AC:Adonor_gain1.0000
3:46898857:CGTG:Cdonor_loss1.0000
3:46898858:G:GGdonor_gain1.0000
3:46898859:TGAG:Tdonor_loss1.0000
3:46898862:G:GGdonor_gain1.0000
3:46899301:AGGCG:Aacceptor_gain1.0000
3:46899302:GGCGG:Gacceptor_gain1.0000
3:46899343:T:TAacceptor_gain1.0000
3:46899344:G:Aacceptor_gain1.0000
3:46899422:G:GTdonor_gain1.0000
3:46899425:G:GGdonor_gain1.0000
3:46899454:GGG:Gdonor_gain1.0000
3:46899455:GG:Gdonor_gain1.0000

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000029695 (3:46878053 G>A), RS1000163329 (3:46901900 G>A,T), RS1000189912 (3:46896501 G>T), RS1000199896 (3:46896910 G>A,T), RS1000204445 (3:46883804 G>A,C), RS1000318629 (3:46878350 C>G), RS1000348133 (3:46876885 G>A), RS1000422134 (3:46884134 C>T), RS1000543742 (3:46882418 G>A,T), RS1000733669 (3:46894896 TA>T,TAA), RS1000754682 (3:46890077 A>G), RS1000812731 (3:46903309 C>T), RS1001284 (3:46892470 C>G), RS1001332385 (3:46883451 A>G,T), RS1001357221 (3:46891386 A>G,T)

Disease associations

OMIM: gene MIM:168468 | disease phenotypes: MIM:125350, MIM:156400, MIM:215045, MIM:600002, MIM:113300

GenCC curated gene-disease

DiseaseClassificationInheritance
chondrodysplasia Blomstrand typeDefinitiveAutosomal recessive
primary failure of tooth eruptionDefinitiveAutosomal dominant
metaphyseal chondrodysplasia, Jansen typeDefinitiveAutosomal dominant
Eiken syndromeStrongAutosomal recessive

Mondo (9): primary failure of tooth eruption (MONDO:0007434), metaphyseal chondrodysplasia, Jansen type (MONDO:0007982), chondrodysplasia Blomstrand type (MONDO:0008970), Eiken syndrome (MONDO:0010803), connective tissue disorder (MONDO:0003900), pseudohypoparathyroidism (MONDO:0019992), brachydactyly type E1 (MONDO:0007223), skeletal dysplasia (MONDO:0018230), intellectual disability (MONDO:0001071)

Orphanet (9): Metaphyseal chondrodysplasia, Jansen type (Orphanet:33067), Primary failure of tooth eruption (Orphanet:412206), Blomstrand lethal chondrodysplasia (Orphanet:50945), Eiken syndrome (Orphanet:79106), Pseudohypoparathyroidism type 1A (Orphanet:79443), Pseudohypoparathyroidism (Orphanet:97593), Brachydactyly type E (Orphanet:93387), Primary bone dysplasia (Orphanet:364526), NON RARE IN EUROPE: Unexplained intellectual disability (Orphanet:319658)

HPO phenotypes

179 total (30 of 179 shown, HPO-id order):

HPOTerm
HP:0000006Autosomal dominant inheritance
HP:0000007Autosomal recessive inheritance
HP:0000121Nephrocalcinosis
HP:0000179Thick lower lip vermilion
HP:0000218High palate
HP:0000248Brachycephaly
HP:0000256Macrocephaly
HP:0000268Dolichocephaly
HP:0000272Malar flattening
HP:0000278Retrognathia
HP:0000293Full cheeks
HP:0000316Hypertelorism
HP:0000322Short philtrum
HP:0000324Facial asymmetry
HP:0000336Prominent supraorbital ridges
HP:0000340Sloping forehead
HP:0000343Long philtrum
HP:0000347Micrognathia
HP:0000365Hearing impairment
HP:0000369Low-set ears
HP:0000405Conductive hearing impairment
HP:0000431Wide nasal bridge
HP:0000452Choanal stenosis
HP:0000453Choanal atresia
HP:0000463Anteverted nares
HP:0000494Downslanted palpebral fissures
HP:0000506Telecanthus
HP:0000508Ptosis
HP:0000518Cataract
HP:0000520Proptosis

GWAS associations

16 associations (top):

StudyTraitp-value
GCST003253_12Microalbuminuria5.000000e-06
GCST005146_44Birth weight1.000000e-08
GCST006867_21Type 2 diabetes2.000000e-08
GCST007388_27Insomnia symptoms (never/rarely vs. usually)6.000000e-08
GCST008362_101Birth weight1.000000e-09
GCST008362_207Birth weight4.000000e-10
GCST008363_105Offspring birth weight1.000000e-08
GCST008363_32Offspring birth weight9.000000e-07
GCST010002_422Refractive error4.000000e-14
GCST012227_986Hip circumference adjusted for BMI2.000000e-08
GCST90020025_1940Waist-to-hip ratio adjusted for BMI9.000000e-13
GCST90020025_1941Waist-to-hip ratio adjusted for BMI1.000000e-11
GCST90020027_171Waist-hip index2.000000e-12
GCST90020027_172Waist-hip index3.000000e-11
GCST90020028_795Hip circumference adjusted for BMI2.000000e-09
GCST90020028_796Hip circumference adjusted for BMI1.000000e-10

EFO canonical traits (5, from GWAS)

EFO IDTrait name
EFO:0004344birth weight
EFO:0007876insomnia measurement
EFO:0005939parental genotype effect measurement
EFO:0008039BMI-adjusted hip circumference
EFO:0007788BMI-adjusted waist-hip ratio

MeSH disease descriptors (8)

DescriptorNameTree numbers
D003240Connective Tissue DiseasesC17.300
D008607Intellectual DisabilityC10.597.606.360; C23.888.592.604.646; F01.700.687; F03.625.539
D011547PseudohypoparathyroidismC05.116.198.709; C16.320.565.618.815; C18.452.104.709; C18.452.174.766; C18.452.648.618.815
C566194Brachydactyly, Type E (supp.)
C537914Chondrodysplasia, blomstrand type (supp.)
C564010Eiken Skeletal Dysplasia (supp.)
C565114Failure of Tooth Eruption, Primary (supp.)
C537564Jansen type metaphyseal chondrodysplasia (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL1793 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

3 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 3,571 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL3301581ABALOPARATIDE4
CHEMBL525610TERIPARATIDE43,549
CHEMBL3976807PCO-371122

PharmGKB: 1 entry (VIP=true, CPIC=false)

PharmGKB variants

1 variants.

VariantGenesLevelScore#Clin annotsDrugs
rs1138518PTH1R0.000

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: gpcr — Parathyroid hormone receptors

Most potent curated ligand interactions (43 total), top 25:

LigandActionAffinityParameter
eneboparatideAgonist10.0pIC50
[Ala1,12,Aib3,Gln10,hArg11,Trp14,Arg19]PTH-(1-34)-NH2Full agonist8.7pIC50
[Arg19]PTH-(1-34) (human)Full agonist8.6pIC50
[Ala1,12,Aib3,Gln10,hArg11,Trp14,Arg19]PTH-(1-28)-NH2 (human)Full agonist8.6pIC50
[Tyr34]PTH-(1-34) (human)Full agonist8.5pIC50
[Ile5]PTHrP-(1-34) (human)Full agonist8.4pIC50
[Tyr34]PTH-(1-34)-NH2 (human)Full agonist8.2pIC50
TIP39-(7-39) (human/bovine)Antagonist8.2pIC50
[Nle8,18,Tyr34]PTH-(1-34)-NH2 (bovine)Full agonist8.1pIC50
PTHrP-(1-34) (human)Full agonist8.1pIC50
PTHrP-(1-20)/TIP-(23-39) (human)Full agonist8.0pIC50
[125I][Nle8,21,Tyr34]PTH-(1-34)-NH2 (rat)Full agonist8.0pKd
[Ile5,Glu19]PTHrP-(1-34) (human)Full agonist8.0pIC50
[Nle8,18,Tyr34]PTH-(3-34)-NH2 (bovine)Full agonist8.0pIC50
[Ile5,Trp23]PTHrP-(1-36) (human)Full agonist7.8pIC50
[Ile5,Trp23]PTHrP-(3-36) (human)Full agonist7.8pIC50
[Ile5,Val21]PTHrP-(1-34) (human)Full agonist7.8pIC50
[Tyr34]PTH-(3-34)-NH2 (human)Full agonist7.8pIC50
PTHrP-(1-21)/PTH-(22-34) (human)Full agonist7.7pIC50
[Ile5,Trp23]PTHrP-(2-36) (human)Full agonist7.6pIC50
[Ile5,Trp23,Tyr36]PTHrP-(1-36)-NH2 (human)Full agonist7.5pIC50
teriparatideFull agonist7.4pIC50
[Ile5,Glu19,Val21]PTHrP-(1-34) (human)Full agonist7.4pIC50
[Ile5,Trp23]PTHrP-(4-36) (human)Full agonist7.4pIC50
[Ile5]PTHrP-(1-36) (human)Full agonist7.4pIC50

ChEMBL bioactivities

156 potent at pChembl≥5 of 176 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
10.70EC500.02nMABALOPARATIDE
10.22EC500.06nMCHEMBL4098420
10.22EC500.06nMCHEMBL526530
10.15EC500.07nMCHEMBL4080397
10.10EC500.08nMCHEMBL4060034
10.10IC500.08nMTERIPARATIDE
9.92EC500.12nMCHEMBL4090619
9.89EC500.13nMCHEMBL4106296
9.85EC500.14nMCHEMBL4088173
9.82EC500.15nMCHEMBL4061182
9.82EC500.15nMCHEMBL506126
9.77EC500.17nMCHEMBL4106296
9.77EC500.17nMCHEMBL4098344
9.74EC500.18nMCHEMBL4074628
9.70EC500.2nMCHEMBL1276264
9.59EC500.26nMCHEMBL4063722
9.57EC500.27nMCHEMBL4097998
9.54EC500.29nMCHEMBL4063322
9.52EC500.3nMTERIPARATIDE
9.49EC500.32nMCHEMBL4106303
9.47EC500.34nMCHEMBL4089035
9.47EC500.34nMCHEMBL4073243
9.44EC500.36nMCHEMBL4093590
9.40EC500.4nMCHEMBL4090894
9.36EC500.44nMCHEMBL4106300
9.32EC500.48nMCHEMBL4097878
9.29EC500.51nMCHEMBL4063242
9.29EC500.51nMCHEMBL4059512
9.28EC500.52nMCHEMBL4069902
9.19EC500.65nMCHEMBL4106304
9.15EC500.71nMCHEMBL4083799
9.10EC500.79nMCHEMBL4106302
9.08EC500.83nMCHEMBL4106301
9.04Ki0.912nMCHEMBL244325
9.04EC500.92nMCHEMBL526677
9.00EC501nMTERIPARATIDE
8.96EC501.1nMCHEMBL525069
8.95EC501.12nMCHEMBL4060554
8.90Kd1.259nMCHEMBL276472
8.90Kd1.259nMCHEMBL439458
8.90Kd1.259nMCHEMBL424859
8.84Ki1.445nMCHEMBL389783
8.74EC501.8nMCHEMBL4090161
8.74Ki1.82nMCHEMBL389787
8.73EC501.84nMCHEMBL4106298
8.66EC502.2nMCHEMBL506126
8.62EC502.4nMCHEMBL1276262
8.60EC502.5nMTERIPARATIDE
8.60EC502.5nMCHEMBL4473665
8.59EC502.59nMCHEMBL4098506

PubChem BioAssay actives

155 with measured affinity, of 353 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

CompoundAssayTypeValueUnit
(4S)-4-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-aminopropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-carboxypropanoyl]amino]hexanoyl]amino]acetyl]amino]hexanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]-5-[[(2S,3S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-amino-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0001uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(1S,2S)-2-aminocyclopentanecarbonyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0001uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(3R)-3-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(3S)-3-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-4-(1H-indol-3-yl)butanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-5-methylsulfanylpentanoyl]amino]-4-carboxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-methylbutanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3S)-7-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2R)-4-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-4-amino-4-oxo-1-phenylbutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-carboxy-4-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxoheptan-3-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-6-oxohexanoic acid1584429: Agonist activity at PTH1 receptor (unknown origin) assessed as induction of cAMPec500.0001uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(1S,2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(1S,2S)-2-aminocyclopentanecarbonyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]cyclopentanecarbonyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0001uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(1S,2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]cyclopentanecarbonyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0001uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(3R)-3-amino-4-hydroxybutanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0001uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(1S)-1-carboxy-2-phenylethyl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-oxopentanoic acid1381232: Displacement of 125I-PTH (1 to 15 residues) from human PTHR1 expressed in African green monkey COS7 cell membranes at 300 uM after 90 mins by gamma counting analysisic500.0001uM
(4S)-5-[[(2S,3S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-6-(diaminomethylideneamino)-1-oxohexan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-[[2-[[(2S)-2-[(2-amino-2-methylpropanoyl)amino]-3-methylbutanoyl]amino]-2-methylpropanoyl]amino]-5-oxopentanoic acid357671: Activity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assayec500.0001uM
(4S)-5-[[(2S,3S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-[[2-[[(2S)-2-[(2-amino-2-methylpropanoyl)amino]-3-methylbutanoyl]amino]-2-methylpropanoyl]amino]-5-oxopentanoic acid357671: Activity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assayec500.0001uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0001uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(3S,4R)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(1S,2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(1S,2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-aminopropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-carboxypropanoyl]amino]hexanoyl]amino]acetyl]amino]hexanoyl]amino]cyclopentanecarbonyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-3-carboxypropanoyl]amino]cyclopentanecarbonyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]pyrrolidine-3-carbonyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-[[(3R,4S)-4-[[(2S)-1-[[(2S)-1-[[1-[[(1S,2S)-2-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(1S,2S)-2-carbamoylcyclopentyl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]cyclopentyl]amino]-2-methyl-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidin-3-yl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0002uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(1S,2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]cyclopentanecarbonyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0002uM
(4S)-5-[[(2S,3S)-1-[[(3S,6S,9S,12S,15S)-3-[[(2S)-1-amino-6-(diaminomethylideneamino)-1-oxohexan-2-yl]carbamoyl]-9-butyl-6-(1H-imidazol-5-ylmethyl)-12-(2-methylpropyl)-5,8,11,14,18,23-hexaoxo-1,17-dioxa-4,7,10,13-tetrazacyclotricos-15-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-[[2-[[(2S)-2-[(2-amino-2-methylpropanoyl)amino]-3-methylbutanoyl]amino]-2-methylpropanoyl]amino]-5-oxopentanoic acid536878: Agonist activity at recombinant PTHR1 expressed in HEK293 cells co-transfected with CRE-Luc assessed as increase of adenylyl cyclase activity after 4.5 hrs by luciferase assayec500.0002uM
(4S)-4-[[(1S,2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(1S,2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]cyclopentanecarbonyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]cyclopentanecarbonyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(3R,4S)-4-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3R,4S)-4-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(1S,2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(1S,2S)-2-carbamoylcyclopentyl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]carbamoyl]cyclopentyl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-3-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]carbamoyl]pyrrolidin-3-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0003uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(3R)-3-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0003uM
(4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(1S,2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]cyclopentanecarbonyl]amino]-4-methylpentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0003uM
(4S)-5-[[(2S,3S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-6-carbamimidamido-1-oxohexan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-aminopropanoyl]amino]-3-methylbutanoyl]amino]propanoyl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0003uM
(4S)-4-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(3S)-7-amino-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(3S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(3S)-3-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(3R)-3-[[(2S)-6-amino-2-[[2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-aminopropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-carboxypropanoyl]amino]hexanoyl]amino]acetyl]amino]hexanoyl]amino]-4-hydroxybutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-3-carboxypropanoyl]amino]-5-methylhexanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-phenylbutanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]heptanoyl]amino]-4-methylpentanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]-6-[[(2S,3S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-4-amino-4-oxobutan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-6-oxohexanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0003uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(1S,2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]cyclopentanecarbonyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0003uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(1S,2S)-2-[[(2S)-5-amino-2-[[(1S,2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(1S,2S)-2-aminocyclopentanecarbonyl]amino]-3-methylbutanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]cyclopentanecarbonyl]amino]-5-oxopentanoyl]amino]cyclopentanecarbonyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-oxopentanoyl]amino]-6-carbamimidamidohexanoyl]amino]propanoyl]amino]hexanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-methylbutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0004uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(3S,4R)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(1S,2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(1S,2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(1S,2S)-2-[[(2S)-5-amino-2-[[(1S,2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(1S,2S)-2-aminocyclopentanecarbonyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]cyclopentanecarbonyl]amino]-5-oxopentanoyl]amino]cyclopentanecarbonyl]amino]-4-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-carboxypropanoyl]amino]hexanoyl]amino]acetyl]amino]hexanoyl]amino]cyclopentanecarbonyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-3-carboxypropanoyl]amino]cyclopentanecarbonyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]pyrrolidine-3-carbonyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-[[(3R,4S)-4-[[(2S)-1-[[(2S)-1-[[1-[[(1S,2S)-2-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(1S,2S)-2-carbamoylcyclopentyl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]cyclopentyl]amino]-2-methyl-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidin-3-yl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0004uM
(4S)-6-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3S)-7-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2R)-4-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-4-amino-4-oxo-1-phenylbutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-carboxy-4-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxoheptan-3-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(3R)-3-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(3S)-3-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-aminopropanoyl]amino]-3-methylbutanoyl]amino]propanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-oxopentanoyl]amino]-6-carbamimidamidohexanoyl]amino]propanoyl]amino]hexanoyl]amino]-4-(1H-indol-3-yl)butanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-5-methylsulfanylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-methylbutanoyl]amino]-6-oxohexanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0004uM
(4S)-5-[[(1S,2S)-2-[[(2S)-5-amino-1-[[(1S,2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[2-[[(2S)-6-amino-1-[[(1S,2S)-2-[[(2S,3S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(1S,2S)-2-[[(2S)-5-carbamimidamido-1-[[(2S)-5-carbamimidamido-1-[[(2S)-5-carbamimidamido-1-[[(3R,4S)-4-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3R,4S)-4-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(1S,2S)-2-[[(2S,3S)-1-[[(2S)-1-[[(2S,3R)-1-[[(1S,2S)-2-carbamoylcyclopentyl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]carbamoyl]cyclopentyl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidin-3-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamoyl]pyrrolidin-3-yl]amino]-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]carbamoyl]cyclopentyl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]carbamoyl]cyclopentyl]amino]-1-oxohexan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]cyclopentyl]amino]-1,5-dioxopentan-2-yl]carbamoyl]cyclopentyl]amino]-4-[[(2S)-2-[[(2S)-2-[[(1S,2S)-2-aminocyclopentanecarbonyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0005uM
(4S)-5-[[(2S,3S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(1S,2S)-2-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(1S,2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3R,4S)-4-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3R,4S)-4-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(1S,2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(1S,2S)-2-carbamoylcyclopentyl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]carbamoyl]cyclopentyl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-3-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]carbamoyl]pyrrolidin-3-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]cyclopentyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]cyclopentyl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-6-carbamimidamido-1-oxohexan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-aminopropanoyl]amino]-3-methylbutanoyl]amino]propanoyl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0005uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(1S,2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(1S,2S)-2-aminocyclopentanecarbonyl]amino]-3-methylbutanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]cyclopentanecarbonyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-oxopentanoyl]amino]-6-carbamimidamidohexanoyl]amino]propanoyl]amino]hexanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-methylbutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0005uM
(4S)-5-[[(1S,2S)-2-[[(2S)-5-amino-1-[[(1S,2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(1S,2S)-2-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(1S,2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3R,4S)-4-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3R,4S)-4-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(1S,2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(1S,2S)-2-carbamoylcyclopentyl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]carbamoyl]cyclopentyl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-3-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]carbamoyl]pyrrolidin-3-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]cyclopentyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]cyclopentyl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-6-carbamimidamido-1-oxohexan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]carbamoyl]cyclopentyl]amino]-1,5-dioxopentan-2-yl]carbamoyl]cyclopentyl]amino]-4-[[2-[[(2S)-2-[[(1S,2S)-2-aminocyclopentanecarbonyl]amino]-3-methylbutanoyl]amino]-2-methylpropanoyl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0005uM
(4S)-5-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[2-[[(2S)-6-amino-1-[[(1S,2S)-2-[[(2S,3S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(1S,2S)-2-[[(2S)-5-carbamimidamido-1-[[(2S)-5-carbamimidamido-1-[[(2S)-5-carbamimidamido-1-[[(3R,4S)-4-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3R,4S)-4-[[(2S)-1-[[(2R,3S)-1-[[(2S)-1-[[(1S,2S)-2-[[(2S,3S)-1-[[(2S)-1-[[(2S,3R)-1-[[(1S,2S)-2-carbamoylcyclopentyl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]carbamoyl]cyclopentyl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidin-3-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamoyl]pyrrolidin-3-yl]amino]-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]carbamoyl]cyclopentyl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]carbamoyl]cyclopentyl]amino]-1-oxohexan-2-yl]amino]-2-oxoethyl]amino]-1-oxohexan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-aminopropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0006uM
(4S)-4-[[(1S,2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(1S,2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(1S,2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(1S,2S)-2-aminocyclopentanecarbonyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]cyclopentanecarbonyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]cyclopentanecarbonyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]cyclopentanecarbonyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(3R,4S)-4-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3R,4S)-4-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(1S,2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(1S,2S)-2-carbamoylcyclopentyl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]carbamoyl]cyclopentyl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-3-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]carbamoyl]pyrrolidin-3-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0007uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(3R)-3-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(3S)-3-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(1S,2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(1S,2S)-2-aminocyclopentanecarbonyl]amino]-3-methylbutanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]cyclopentanecarbonyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-oxopentanoyl]amino]-6-carbamimidamidohexanoyl]amino]propanoyl]amino]hexanoyl]amino]-4-(1H-indol-3-yl)butanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-5-methylsulfanylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-methylbutanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3S)-7-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2R)-4-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-4-amino-4-oxo-1-phenylbutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-carboxy-4-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxoheptan-3-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-6-oxohexanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0008uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(3R)-3-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(3S)-3-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(1S,2S)-2-[[(2S)-5-amino-2-[[(1S,2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(1S,2S)-2-aminocyclopentanecarbonyl]amino]-3-methylbutanoyl]amino]-2-methylpropanoyl]amino]-4-carboxybutanoyl]amino]cyclopentanecarbonyl]amino]-5-oxopentanoyl]amino]cyclopentanecarbonyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-oxopentanoyl]amino]-6-carbamimidamidohexanoyl]amino]propanoyl]amino]hexanoyl]amino]-4-(1H-indol-3-yl)butanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-5-methylsulfanylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-methylbutanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3S)-7-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2R)-4-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-4-amino-4-oxo-1-phenylbutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-carboxy-4-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxoheptan-3-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-6-oxohexanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0008uM
5-cyclohexyl-1-[4-[2-(1H-imidazol-2-yl)ethylamino]phenyl]-8-methyl-3-(6,7,8,9-tetrahydro-5H-benzo[7]annulen-7-yl)-1,3,4-benzotriazepin-2-one298267: Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellski0.0009uM
(4S)-5-[[(2S,3S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-6-[[2-(3-hydroxy-6-oxoxanthen-9-yl)benzoyl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-[[2-[[(2S)-2-[(2-amino-2-methylpropanoyl)amino]-3-methylbutanoyl]amino]-2-methylpropanoyl]amino]-5-oxopentanoic acid357671: Activity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assayec500.0009uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(3S)-3-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-5-methylhexanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0011uM
(4S)-5-[[(2S,3S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-amino-6-[[2-(3-hydroxy-6-oxoxanthen-9-yl)benzoyl]amino]-1-oxohexan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-[[2-[[(2S)-2-[(2-amino-2-methylpropanoyl)amino]-3-methylbutanoyl]amino]-2-methylpropanoyl]amino]-5-oxopentanoic acid357671: Activity at human PTH/PTH-related peptide receptor expressed in HEK293 cells assessed as induction of luciferase activity by CRE-luciferase reporter assayec500.0011uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(Z,2R,5S)-5-amino-4-chloro-2-propan-2-ylhex-3-enoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-oxopentanoic acid1572991: Binding affinity to human PTH receptor expressed in OK-1 cellskd0.0013uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(Z,2R,5S)-5-amino-4-fluoro-2-propan-2-ylhex-3-enoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-oxopentanoic acid1572991: Binding affinity to human PTH receptor expressed in OK-1 cellskd0.0013uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(Z,2R,5S)-5-amino-4-chloro-2-methylhex-3-enoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-oxopentanoic acid1572991: Binding affinity to human PTH receptor expressed in OK-1 cellskd0.0013uM
7-(benzylamino)-5-cyclohexyl-1-[4-[2-(1H-imidazol-2-yl)ethylamino]phenyl]-3,8-dimethyl-1,3,4-benzotriazepin-2-one298267: Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellski0.0014uM
(4S)-5-[[(2S,3S)-1-[[(2S)-5-amino-1-[[(1S,2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(1S,2S)-2-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(1S,2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3R,4S)-4-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3R,4S)-4-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(1S,2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(1S,2S)-2-carbamoylcyclopentyl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]carbamoyl]cyclopentyl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-3-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]carbamoyl]pyrrolidin-3-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]cyclopentyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]carbamoyl]cyclopentyl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-6-carbamimidamido-1-oxohexan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]carbamoyl]cyclopentyl]amino]-1,5-dioxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-[[2-[[(2S)-2-[[(1S,2S)-2-aminocyclopentanecarbonyl]amino]-3-methylbutanoyl]amino]-2-methylpropanoyl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0018uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(3R)-3-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(3S)-3-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(1S,2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(1S,2S)-2-aminocyclopentanecarbonyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]cyclopentanecarbonyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-4-(1H-indol-3-yl)butanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-5-methylsulfanylpentanoyl]amino]-4-carboxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-methylbutanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3S)-7-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2R)-4-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-4-amino-4-oxo-1-phenylbutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-carboxy-4-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxoheptan-3-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-6-oxohexanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0018uM
5-cyclohexyl-1-[4-[2-(1H-imidazol-2-yl)ethylamino]phenyl]-3,8-dimethyl-7-phenylmethoxy-1,3,4-benzotriazepin-2-one298267: Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellski0.0018uM
(4S)-5-[[(2S,3S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-amino-6-(diaminomethylideneamino)-1-oxohexan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-[[2-[[(2S)-2-[(2-amino-2-methylpropanoyl)amino]-3-methylbutanoyl]amino]-2-methylpropanoyl]amino]-5-oxopentanoic acid536878: Agonist activity at recombinant PTHR1 expressed in HEK293 cells co-transfected with CRE-Luc assessed as increase of adenylyl cyclase activity after 4.5 hrs by luciferase assayec500.0024uM
(4S)-4-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(1S)-1-carboxy-2-phenylethyl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-oxopentanoic acid1547045: Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIAec500.0025uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(3R,4S)-3-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-4-methylhexanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0026uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(1S,2S)-2-[[(2S)-5-amino-2-[[(1S,2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(1S,2S)-2-aminocyclopentanecarbonyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]cyclopentanecarbonyl]amino]-5-oxopentanoyl]amino]cyclopentanecarbonyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0030uM
5-cyclohexyl-1-[4-[2-(1H-imidazol-2-yl)ethylamino]phenyl]-8-methyl-3-propan-2-yl-1,3,4-benzotriazepin-2-one298267: Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellski0.0035uM
3-benzyl-5-cyclohexyl-1-[4-[2-(1H-imidazol-2-yl)ethylamino]phenyl]-8-methyl-1,3,4-benzotriazepin-2-one298267: Displacement of [125I]-[Nle,8,18 Tyr34]-hPTH(1-34) from human recombinant PTH1R expressed in HEK293 cellski0.0038uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(3S)-3-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(3R)-3-[[(2S)-6-amino-2-[[2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-aminopropanoyl]amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-carboxypropanoyl]amino]hexanoyl]amino]acetyl]amino]hexanoyl]amino]-4-hydroxybutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-3-carboxypropanoyl]amino]-5-methylhexanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(3S)-7-amino-1-[[(2S)-1-[[(2S)-1-[[1-[[(3S)-7-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-4-amino-4-oxobutan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxoheptan-3-yl]amino]-2-methyl-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxoheptan-3-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-6-oxohexanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0041uM
(4S)-5-[[(2S,3S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[2-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-[[(3R)-3-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-3-methylbutanoyl]amino]-4-hydroxybutanoyl]amino]-5-oxopentanoic acid1471701: Agonist activity at human PTH1 receptor expressed in human GP2.3 cells assessed as induction of cAMP after 12 to 20 mins by luciferase reporter gene assayec500.0050uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(Z,2R,5S)-5-amino-4-fluoro-2-methylhex-3-enoyl]amino]-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]hexanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-oxopentanoic acid1572991: Binding affinity to human PTH receptor expressed in OK-1 cellskd0.0063uM

CTD chemical–gene interactions

33 total (human), top 30 by PubMed support.

ChemicalActions (top 5)PubMed papers
Valproic Acidincreases expression, affects expression, increases methylation, affects cotreatment4
sodium arseniteaffects splicing, decreases expression, increases expression2
Benzo(a)pyrenedecreases expression, increases methylation2
Estradiolaffects binding, increases expression2
Aflatoxin B1decreases expression, decreases methylation2
FR900359decreases phosphorylation1
daidzeinaffects cotreatment, affects expression1
methyleugenoldecreases expression1
bisphenol Aaffects cotreatment, increases expression1
daidzinaffects cotreatment, affects expression1
genistinaffects cotreatment, affects expression1
perfluorooctane sulfonic acidincreases expression1
glyciteinaffects cotreatment, affects expression1
perfluoro-n-nonanoic acidincreases expression1
glycitinaffects cotreatment, affects expression1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamideaffects cotreatment, increases expression1
dorsomorphinaffects cotreatment, increases expression1
bisphenol Sdecreases methylation1
Zoledronic Aciddecreases expression1
Air Pollutantsdecreases expression, increases abundance1
Arsenicaffects methylation1
Calcitrioldecreases expression1
Cytarabinedecreases expression1
Dexamethasoneaffects cotreatment, increases expression1
Endosulfanincreases expression1
Indomethacinaffects cotreatment, increases expression1
Leadaffects expression1
Dronabinoldecreases expression1
Tobacco Smoke Pollutionincreases expression1
1-Methyl-3-isobutylxanthineaffects cotreatment, increases expression1

ChEMBL screening assays

59 unique, capped per target: 42 functional, 17 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1050759FunctionalAgonist activity at PTHREleven amino acid glucagon-like peptide-1 receptor agonists with antidiabetic activity. — J Med Chem
CHEMBL1259303BindingActivation of human PTH1 receptorDiscovery of a class of calcium sensing receptor positive allosteric modulators; 1-(benzothiazol-2-yl)-1-phenylethanols. — Bioorg Med Chem Lett

Cellosaurus cell lines

8 cell lines: 4 spontaneously immortalized cell line, 2 transformed cell line, 2 cancer cell line

First 10 cell lines (id-ordered, not curated):

CellosaurusNameCategorySex
CVCL_A8QRUAMS-32PSpontaneously immortalized cell lineSex unspecified
CVCL_C0TPACTOne PTHR1Transformed cell lineFemale
CVCL_H497CHO-K1/PTH1/Galpha15Spontaneously immortalized cell lineFemale
CVCL_KA75HEK293/PTHR1/CRE/beta-lactamaseTransformed cell lineFemale
CVCL_KV70cAMP Hunter CHO-K1 PTHR1 Gs/GqSpontaneously immortalized cell lineFemale
CVCL_KY90PathHunter CHO-K1 PTHR1 beta-arrestinSpontaneously immortalized cell lineFemale
CVCL_LB24PathHunter U2OS PTHR1 Activated GPCR InternalizationCancer cell lineFemale
CVCL_TH52HAP1 PTH1R (-)Cancer cell lineMale

Clinical trials (associated diseases)

294 trials via MONDO — disease-level, not drug-specific.

TrialPhaseStatusTitle
NCT01042158PHASE4COMPLETEDA Clinical Trial of Ambrisentan and Tadalafil in Pulmonary Arterial Hypertension Associated With Systemic Sclerosis
NCT03688191PHASE4UNKNOWNStudy of Sirolimus in CTD-TP in China
NCT04169100PHASE4UNKNOWNNovel Form of Acquired Long QT Syndrome
NCT04197050PHASE4UNKNOWNEffect of Sacubitril/Valsartan on Reduced Right Ventricular Ejection Fraction in Patients With CTD
NCT04928586PHASE4UNKNOWNImmunosuppressant Combined With Pirfenidone in CTD-ILD
NCT05440240PHASE4RECRUITINGPercutaneous Needle Fasciotomy +/- Corticosteroid Injection for Dupuytren’s Contracture
NCT05505409PHASE4UNKNOWNEfficacy and Safety of Pirfenidone in CTD-ILD
NCT06499233PHASE4RECRUITINGEfficacy and Safety of Prophylactic Treatment for Pneumocystis Jirovecii Pneumonia in Patients With Autoimmune Inflammatory Rheumatic Disease
NCT05657860PHASE4COMPLETEDGuanfacine Extended Release for the Reduction of Aggression and Self-injurious Behavior Associated With Prader-Willi Syndrome
NCT05744479PHASE4RECRUITINGMetformin for Antipsychotic-induced Weight Gain in Adults With Intellectual Disability
NCT06107829PHASE4WITHDRAWNValbenazine Treatment of Tardive Dyskinesia in Adults With Intellectual/Developmental Disabilities
NCT06997198PHASE4NOT_YET_RECRUITINGDeutetrabenazine Treatment for Tardive Dyskinesia in Intellectual/Developmental Disabilities
NCT00864201PHASE3UNKNOWNA Study to Evaluate the Use of Bosentan in Patients With Exercise Induced Pulmonary Arterial Hypertension Associated With Connective Tissue Disease
NCT01196091PHASE3COMPLETEDA Study of LY2127399 in Participants With Systemic Lupus Erythematosus
NCT01205438PHASE3COMPLETEDA Study of LY2127399 in Participants With Systemic Lupus Erythematosus
NCT01488708PHASE3TERMINATEDOn Open-Label Study in Participants With Systemic Lupus Erythematosus
NCT03626688PHASE3COMPLETEDA Study Evaluating the Efficacy and Safety of Ralinepag to Improve Treatment Outcomes in PAH Patients
NCT03683186PHASE3ENROLLING_BY_INVITATIONA Study Evaluating the Long-Term Efficacy and Safety of Ralinepag in Subjects With PAH Via an Open-Label Extension
NCT04084678PHASE3TERMINATEDA Study of Ralinepag to Evaluate Effects on Exercise Capacity by CPET in Subjects With WHO Group 1 PH
NCT06716606PHASE3RECRUITINGA Study to Investigate the Long-term Safety and Efficacy of Belimumab in Adults With Interstitial Lung Disease (ILD) Associated With Systemic Sclerosis (SSc) and Other Connective Tissue Diseases (CTD) (BLISSconneCTD-OLE)
NCT06917690PHASE3RECRUITINGA Study to Learn About the Safety and Efficacy of the Drug Oleogel-S10 in Japanese Patients With Epidermolysis Bullosa
NCT02270736PHASE3COMPLETEDClinical Study to Investigate the Efficacy and Safety of NT 201 Compared to Placebo in the Treatment of Chronic Troublesome Drooling Associated With Neurological Disorders and/or Intellectual Disability
NCT00004357PHASE2COMPLETEDAbsorption of Corticosteroids in Children With Juvenile Dermatomyositis
NCT00005675PHASE2COMPLETEDOral Type I Collagen for Relieving Scleroderma
NCT01808196PHASE2COMPLETEDTesting Effectiveness of Losartan in Patients With EoE With or Without a CTD
NCT02682511PHASE2ACTIVE_NOT_RECRUITINGOral Ifetroban to Treat Diffuse Cutaneous Systemic Sclerosis (SSc) or SSc-associated Pulmonary Arterial Hypertension
NCT04993885PHASE2RECRUITINGAvatrombopag in the Treatment of Adult Immune Thrombocytopenia With Autoantibodies
NCT05516758PHASE2TERMINATEDA Study of Peresolimab (LY3462817) in Participants With Moderately-to-Severely Active Rheumatoid Arthritis
NCT05998759PHASE2RECRUITINGTelitacicept for the Treatment of Connective Tissue Disease-associated Thrombocytopenia
NCT06104228PHASE2RECRUITING129 Xenon MRI as a Biomarker for Diagnosis and Response to Therapy in Pulmonary Arterial Hypertension (PAH)
NCT03029429PHASE2ACTIVE_NOT_RECRUITINGTheophylline Treatment for Pseudohypoparathyroidism
NCT04240821PHASE2ENROLLING_BY_INVITATIONTheophylline for Treatment of Pseudohypoparathyroidism
NCT04551170PHASE2ACTIVE_NOT_RECRUITINGTheophylline Treatment for Pseudohypoparathyroidism - Children 2-12 Years Old
NCT02304302PHASE2COMPLETEDDown Syndrome Memantine Follow-up Study
NCT03862950PHASE2COMPLETEDA Trial of Metformin in Individuals With Fragile X Syndrome (Met)
NCT04529226PHASE2UNKNOWNStudy to Compare Clozapine vs Treatment as Usual in People With Intellectual Disability & Treatment-resistant Psychosis
NCT04821856PHASE2COMPLETEDEvaluation of the Effectiveness of Cannabidiol in Treating Severe Behavioural Problems in Children and Adolescents With Intellectual Disability
NCT01093911PHASE1COMPLETEDSafety Study of CDP7657 in Healthy Volunteers and Patients With Systemic Lupus Erythematosus (SLE)
NCT01764594PHASE1COMPLETEDSafety Study of CDP7657 in Patients With Systemic Lupus Erythematosus
NCT02392130PHASE1COMPLETEDA Clinical Trial to Assess the Potential of LEO 130852A Gel to Reduce Steroid Induced Skin Atrophy on Healthy Skin

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 80

This page pulls from 80 datasets indexed by BioBTree:

alphafoldalphamissenseantibodybgeebgee_evidencebindingdbbiogrid_interactionbrendabrenda_kineticsccdscellosauruschembl_activitychembl_assaychembl_documentchembl_moleculechembl_targetciviccivic_evidenceclingen_dosageclingen_gene_validityclinical_trialsclinvarcollectrictd_gene_interactiondbsnpdepmapdiamond_similarityefoensemblentrezesm2_similarityexonfantom5_genefantom5_promotergenccgenerifgogoparentgtopdbgtopdb_interactiongwasgwas_studyhgnchpointactinterprointogenjasparmeshmimmirdbmondomsigdborphanetorthologparalogpatent_compoundpdbpfampharmgkb_clinicalpharmgkb_genepharmgkb_guidelinepharmgkb_variantpubchempubchem_activitypubchem_assaypubmedreactomereactomeparentrefseqrhearnacentralscxa_expressionscxa_gene_experimentsignorspliceaistring_interactiontranscriptufeatureuniprot