CRHR1

Summary

CRHR1 (corticotropin releasing hormone receptor 1, HGNC:2357) is a protein-coding gene on chromosome 17q21.31, encoding Corticotropin-releasing factor receptor 1 (P34998). G-protein coupled receptor for CRH (corticotropin-releasing factor) and UCN (urocortin).

This gene encodes a G-protein coupled receptor that binds neuropeptides of the corticotropin releasing hormone family that are major regulators of the hypothalamic-pituitary-adrenal pathway. The encoded protein is essential for the activation of signal transduction pathways that regulate diverse physiological processes including stress, reproduction, immune response and obesity. Alternative splicing results in multiple transcript variants. Naturally-occurring readthrough transcription between this gene and upstream GeneID:147081 results in transcripts that encode isoforms that share similarity with the products of this gene.

Source: NCBI Gene 1394 — RefSeq curated summary.

At a glance

• GWAS associations: 66
• Clinical variants (ClinVar): 104 total — 32 pathogenic, 4 likely-pathogenic
• Druggable target: yes — 6 molecules with ChEMBL bioactivity
• Dosage sensitivity (ClinGen): haploinsufficiency no evidence, triplosensitivity no evidence
• MANE Select transcript: NM_004382

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:2357
Approved symbol	CRHR1
Name	corticotropin releasing hormone receptor 1
Location	17q21.31
Locus type	gene with protein product
Status	Approved
Aliases	CRF-R, CRF1
Ensembl gene	ENSG00000120088
Ensembl biotype	protein_coding
OMIM	122561
Entrez	1394

Gene structure

Transcript identifiers

Ensembl transcripts: 21 — 8 retained_intron, 6 protein_coding, 4 nonsense_mediated_decay, 3 protein_coding_CDS_not_defined

ENST00000314537, ENST00000339069, ENST00000347197, ENST00000352855, ENST00000398285, ENST00000535778, ENST00000577353, ENST00000580876, ENST00000580955, ENST00000581479, ENST00000582766, ENST00000583888, ENST00000619154, ENST00000705340, ENST00000705341, ENST00000705342, ENST00000705343, ENST00000705344, ENST00000705345, ENST00000705346, ENST00000941062

RefSeq mRNA: 6 — MANE Select: NM_004382 NM_001145146, NM_001145147, NM_001145148, NM_001303016, NM_001303020, NM_004382

CCDS: CCDS42350, CCDS45712, CCDS45713, CCDS45714

Canonical transcript exons

ENST00000314537 — 13 exons

Exon	Start	End
ENSE00002684871	45784320	45784577
ENSE00003595121	45816463	45816582
ENSE00003604504	45807010	45807097
ENSE00003993360	45821355	45821440
ENSE00003993365	45829215	45829321
ENSE00003993366	45830094	45830214
ENSE00003993371	45834624	45835828
ENSE00003995529	45833138	45833210
ENSE00003995530	45833714	45833849
ENSE00003995531	45830880	45830940
ENSE00003995532	45830417	45830570
ENSE00003995533	45834007	45834048
ENSE00003995534	45833452	45833537

Expression profiles

Bgee: expression breadth ubiquitous, 113 present calls, max score 94.08.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.6750 / max 61.0640, expressed in 135 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
161302	0.3139	95
161301	0.2879	93
161300	0.0732	36

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
right hemisphere of cerebellum	UBERON:0014890	94.08	gold quality
cerebellar cortex	UBERON:0002129	93.71	gold quality
cerebellar hemisphere	UBERON:0002245	93.70	gold quality
cerebellum	UBERON:0002037	93.67	gold quality
adenohypophysis	UBERON:0002196	85.52	gold quality
right frontal lobe	UBERON:0002810	84.01	gold quality
pituitary gland	UBERON:0000007	83.45	gold quality
superior frontal gyrus	UBERON:0002661	82.83	gold quality
primary visual cortex	UBERON:0002436	82.55	gold quality
Brodmann (1909) area 9	UBERON:0013540	82.55	gold quality
frontal cortex	UBERON:0001870	81.74	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	81.08	gold quality
prefrontal cortex	UBERON:0000451	80.16	gold quality
cerebral cortex	UBERON:0000956	79.34	gold quality
anterior cingulate cortex	UBERON:0009835	77.93	gold quality
brain	UBERON:0000955	77.11	gold quality
temporal lobe	UBERON:0001871	76.13	gold quality
amygdala	UBERON:0001876	75.88	gold quality
cortical plate	UBERON:0005343	75.04	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	73.42	gold quality
Ammon’s horn	UBERON:0001954	72.39	gold quality
hypothalamus	UBERON:0001898	70.92	gold quality
ectocervix	UBERON:0012249	66.55	gold quality
ganglionic eminence	UBERON:0004023	65.99	gold quality
body of uterus	UBERON:0009853	65.03	gold quality
endocervix	UBERON:0000458	64.82	gold quality
substantia nigra	UBERON:0002038	64.64	gold quality
nucleus accumbens	UBERON:0001882	64.42	gold quality
caudate nucleus	UBERON:0001873	64.30	gold quality
putamen	UBERON:0001874	64.26	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-ANND-3	no	0.16

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

1 targets.

Target	Regulation
POMC	Activation

Upstream regulators (CollecTRI, top): AP1, HR, NFKB1, NFKB, NFKBIA, NR4A2, RELA

miRNA regulators (miRDB)

52 targeting CRHR1, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-3689D	100.00	66.14	1181
HSA-MIR-6851-5P	100.00	65.63	1294
HSA-MIR-656-3P	100.00	72.15	2788
HSA-MIR-6870-5P	99.99	68.55	2115
HSA-MIR-34A-5P	99.99	71.21	1784
HSA-MIR-449A	99.99	71.05	1776
HSA-MIR-4723-5P	99.97	68.70	2034
HSA-MIR-5698	99.97	68.49	2029
HSA-MIR-7111-5P	99.97	68.48	2062
HSA-MIR-34C-5P	99.97	70.45	1577
HSA-MIR-449B-5P	99.97	70.26	1580
HSA-MIR-185-3P	99.95	67.01	1743
HSA-MIR-6721-5P	99.93	68.92	2981
HSA-MIR-4697-3P	99.89	67.09	1123
HSA-MIR-577	99.78	69.13	2479
HSA-MIR-4502	99.65	66.99	1021
HSA-MIR-1249-5P	99.61	66.55	2049
HSA-MIR-6797-5P	99.61	66.55	2084
HSA-MIR-6132	99.60	65.83	1554
HSA-MIR-6836-5P	99.60	65.62	1538
HSA-MIR-1207-5P	99.49	69.11	2983
HSA-MIR-4441	99.49	66.56	3216
HSA-MIR-6722-3P	99.45	67.62	1919
HSA-MIR-940	99.37	66.14	2064
HSA-MIR-6808-5P	99.31	66.23	2150
HSA-MIR-6893-5P	99.31	66.25	2119
HSA-MIR-4505	99.27	67.81	2678
HSA-MIR-4685-5P	99.25	65.99	1563
HSA-MIR-6837-5P	99.25	65.47	1632
HSA-MIR-4763-3P	99.10	67.83	2649

Functional genomics

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

Literature-anchored findings (GeneRIF, showing 40)

• CRH inhibits cell growth of human endometrial adenocarcinoma cells via CRH-receptor 1-mediated activation of cAMP-PKA pathway (PMID:11861501)
• The binding of CRF to the type 1 receptor may be involved in regulating the development of cerebellar neurons and glia immediately after birth, before CRF assumes its function as a neuromodulator later in postnatal development and in the adult. (PMID:12504877)
• results showed that CRH-R1 alpha mRNA levels and protein levels were significantly reduced in preeclamptic and growth-restricted placentas (PMID:12519878)
• Detected in placenta, myometrium, decidua, and fetal membranes. Widespread expression of CRH system in gestational tissue suggests paracrine role CRH in birth process (e.g. effects on macrophages and endothelial cells). (PMID:12784189)
• Ser(301), which is located in the third intracellular loop of CRHR1, is critical for efficient coupling of the receptor to G proteins and to second messenger generation. (PMID:14657255)
• CRH-R1:CRH-R2 ratio varied according to fat-depot type; whereas CRH-R1 expression was higher in sc fat than in visceral fat, the opposite was true for CRH-R2. (PMID:14764822)
• This review notes findings that implicate CRF1 receptors in stress-related stimulation of colonic function and hypersensitivity to colorectal distention. (PMID:15100165)
• Cortagine, an agonist of CRF1, modulates depression and anxieety in c57bl mice in maze learning. (PMID:15192151)
• characterization of isoforms and effect on cyclic AMP levels (PMID:15206947)
• coupling of CRFR1 to different G proteins is regulated by concentrations of the stimulating ligand and GTP (PMID:15252011)
• Study found increased response to antidepressants in highly anxious patients homozygous for the GAG haplotype of CRH receptor 1. (PMID:15365580)
• phospholipase C-mediated signaling of CRF receptors is dependent upon the cellular background and that in HEK293 cells human CRF receptors robustly respond in the FLIPR format. (PMID:15450949)
• the CRH-R1alpha carboxyl tail is important for regulation of receptor activity by G protein-coupled receptor kinase (PMID:15498832)
• Pregnancies with abnormal placental function such as preeclampsia are characterized by increased maternal plasma CRH concentrations and reduced placental CRH-receptor 1alpha. (PMID:15784708)
• Chronic urticaria expresses high levels of CRH-R1 as compared to normal foreskin, breast skin and cultured human keratinocytes. (PMID:16297195)
• CRF1alpha receptor resensitization is regulated in an atypical manner by Rab GTPases. (PMID:16412099)
• In adolescents, significant group differences between genotypes were observed in binge drinking and lifetime prevalences of alcohol intake and drunkenness. In adult alcohol-dependent patients, CRHR1 was associated with high amounts of drinking. (PMID:16550213)
• adrenocortical cells exhibit a higher expression of functional CRH receptors than chromaffin cells and that CRH acts on adrenal DHEA production (PMID:16721033)
• expression of CRH-BP, CRH-R1 and CRH-R2 in uterine tissues is down-regulated during pregnancy (PMID:16734917)
• Deletion of CRHR1 is associated with a common inversion polymorphism. (PMID:16906164)
• A complex signaling network appears to mediate CRH-R1alpha-MAPK interactions; PI3-K might play a critical role in the regulation of CRH-R1alpha signaling selectivity and cellular responses. (PMID:16959871)
• our results do not support an involvement of CRHR1 gene in progressive supranuclear palsy pathogenesis (PMID:17010515)
• Both CRHR1 and CRHR2 play a facilitatory role in the non-clathrin-, non-caveolae-mediated endocytosis and intracellular signal transduction of urocortin. (PMID:17170072)
• The results support the idea that the CRHR1 gene is likely to be involved in the antidepressant response in MDD. (PMID:17258395)
• The elevated level of placental CRH may be a trigger of the transcription of its own receptor CRH-R1 during caesarian operations. (PMID:17294739)
• V1bR and CRHR1 can form constitutive homo- and heterodimers. (PMID:17318384)
• affected psoriatic skin has decreased gene expression of CRH-R1 mRNA than normal con (PMID:17330132)
• Stratification based on the levels of lifetime stress showed reproducible association and linkage of an SNP in the CRHR1 gene (rs4792887) to suicide attempters exposed to low levels of stress (P = 0.002), among whom most males were depressed. (PMID:17376150)
• in chorion trophoblast cells, CRHR1 and CRHR2 mediate divergent effects on PGDH expression, and this may provide a precise regulation of PGs levels from chorion to myometrium during pregnancy (PMID:17463062)
• Adolescents homozygous for the C allele of rs1876831 drank higher maximum amounts of alcohol per occasion and had greater lifetime rates of heavy drinking in relation to negative life events than individuals carrying the T allele. (PMID:17597588)
• Findings support the hypothesis that CRHR1 antagonists could potentially be used against ovarian cancer. (PMID:17667919)
• A penta-aminoacid cassette within the 29-aminoacid insert of CRH-R1beta contains multiple positive charged aminoacids, an important structural determinant for the impaired cAMP response and CRH-R1 coupling to Gs proteins. (PMID:17913459)
• Human myometrium expresses both CRH-R1 and CRH-R2 during pregnancy. A heterogeneous distribution of CRH-R1 variants in term labor and nonlabor myometrium might be related to the contractile phenotype of myometrium at term. (PMID:17959885)
• These findings imply that nonpeptide ligands differentially modulate conformational states involved in CRF(1) receptor activation. (PMID:18239030)
• To examine whether the effects of child abuse on adult depressive symptoms are moderated by genetic polymorphisms within the corticotropin-releasing hormone type 1 receptor (CRHR1) gene. (PMID:18250257)
• Cultured placental trophoblasts express both CRH-R1 and CRH-R2. (PMID:18325997)
• polymorphisms in the AVPR1B and the CRHR1 genes alter the susceptibility to panic disorder (PMID:18384079)
• genes encoding corticotropin releasing hormone receptor 1, tachykinin receptor 1, gastrin releasing peptide, and gastrin releasing peptide receptor were selected as candidates for PD based on their biology (PMID:18452185)
• CRHR1 polymorphisms are not associated with immediate or long-term improvement in FEV1 by inhaled corticosteroids (PMID:18539200)
• Three CRHR1 single nucleotide polymorphisms (SNPs), all in linkage disequilibrium, were associated with bone density in a sex-specific manner in ALL survivors. (PMID:18565889)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	crhr1	ENSDARG00000003989
mus_musculus	Crhr1	ENSMUSG00000018634
rattus_norvegicus	Crhr1	ENSRNOG00000004900
drosophila_melanogaster	Dh44-R1	FBGN0033932

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), 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), PTH1R (ENSG00000160801), ADGRL4 (ENSG00000162618), EVA1C (ENSG00000166979), ADGRF3 (ENSG00000173567), ADGRG2 (ENSG00000173698), ADGRE1 (ENSG00000174837), ADGRD2 (ENSG00000180264), ADGRB1 (ENSG00000181790), ADGRG3 (ENSG00000182885), ADGRA1 (ENSG00000197177)

Protein

Protein identifiers

Corticotropin-releasing factor receptor 1 — P34998 (reviewed: P34998)

Alternative names: Corticotropin-releasing hormone receptor 1

All UniProt accessions (6): A0A994J7S2, A0A994J7T2, B3SXS2, P34998, J9JIC6, K9J956

UniProt curated annotations — full annotation on UniProt →

Function. G-protein coupled receptor for CRH (corticotropin-releasing factor) and UCN (urocortin). Has high affinity for CRH and UCN. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and down-stream effectors, such as adenylate cyclase. Promotes the activation of adenylate cyclase, leading to increased intracellular cAMP levels. Inhibits the activity of the calcium channel CACNA1H. Required for normal embryonic development of the adrenal gland and for normal hormonal responses to stress. Plays a role in the response to anxiogenic stimuli.

Subunit / interactions. Heterodimer; heterodimerizes with GPER1. Interacts (via N-terminal extracellular domain) with CRH and UCN. Interacts with DLG1; this inhibits endocytosis of CRHR1 after agonist binding.

Subcellular location. Cell membrane. Endosome.

Tissue specificity. Predominantly expressed in the cerebellum, pituitary, cerebral cortex and olfactory lobe.

Post-translational modifications. C-terminal Ser or Thr residues may be phosphorylated. Phosphorylation at Ser-301 by PKA prevents maximal coupling to Gq-protein, and thereby negatively regulates downstream signaling.

Domain organisation. The transmembrane domain is composed of seven transmembrane helices that are arranged in V-shape. Transmembrane helix 7 assumes a sharply kinked structure. The antagonist CP-376395 binds at an allosteric site, far from the presumed binding site for the physiological peptide ligand.

Miscellaneous. Major isoform. Does not bind to CRF with high affinity.

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

Isoforms (5)

UniProt ID	Names	Canonical?
P34998-2	CRF-R2	yes
P34998-1	CRF-R1
P34998-3	CRF-R3
P34998-4	CRF-R4, 1D
P34998-5	5

RefSeq proteins (6): NP_001138618, NP_001138619, NP_001138620, NP_001289945, NP_001289949, NP_004373* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000832	GPCR_2_secretin-like	Family
IPR001879	GPCR_2_extracellular_dom	Domain
IPR003051	GPCR_2_CRF_rcpt	Family
IPR003052	GPCR_2_CRF1_rcpt	Family
IPR017981	GPCR_2-like_7TM	Domain
IPR017983	GPCR_2_secretin-like_CS	Conserved_site
IPR036445	GPCR_2_extracell_dom_sf	Homologous_superfamily
IPR050332	GPCR_2	Family

Pfam: PF00002, PF02793

UniProt features (67 total): helix 14, mutagenesis site 9, topological domain 8, transmembrane region 7, strand 6, glycosylation site 5, turn 5, disulfide bond 4, splice variant 4, region of interest 2, signal peptide 1, chain 1, modified residue 1

Structure

Experimental structures (PDB)

11 structures.

PDB	Method	Resolution (Å)
3EHU	X-RAY DIFFRACTION	1.96
8GTI	X-RAY DIFFRACTION	2.2
8GTM	X-RAY DIFFRACTION	2.6
8GTG	X-RAY DIFFRACTION	2.75
3EHS	X-RAY DIFFRACTION	2.76
6P9X	ELECTRON MICROSCOPY	2.91
4K5Y	X-RAY DIFFRACTION	2.98
6PB0	ELECTRON MICROSCOPY	3
4Z9G	X-RAY DIFFRACTION	3.18
3EHT	X-RAY DIFFRACTION	3.4
2L27	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P34998-F1	77.84	0.24

Antibody-complex structures (SAbDab): 2 — 6P9X, 6PB0

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): 301

Disulfide bonds (4): 30–54, 44–87, 68–102, 188–258

Glycosylation sites (5): 38, 45, 78, 90, 98

Mutagenesis-validated functional residues (9):

Position	Phenotype
203	nearly abolishes antagonist binding.
206	strongly reduces antagonist binding.
280	nearly abolishes antagonist binding.
283	nearly abolishes antagonist binding.
284	slightly reduces antagonist binding.
287	strongly reduces antagonist binding.
290	strongly reduces antagonist binding.
327	strongly reduces antagonist binding.
355	increases antagonist binding.

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

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

MSigDB gene sets: 237 (showing top): RNGTGGGC_UNKNOWN, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_NEGATIVE_REGULATION_OF_TRANSMEMBRANE_TRANSPORT, GOBP_RESPONSE_TO_ETHANOL, MORF_FLT1, BENPORATH_ES_WITH_H3K27ME3, GOBP_BEHAVIOR, GOBP_NEGATIVE_REGULATION_OF_TRANSPORTER_ACTIVITY, MORF_MSH3, ENK_UV_RESPONSE_KERATINOCYTE_UP, GOBP_ADULT_BEHAVIOR, MORF_BRCA1, GRAESSMANN_APOPTOSIS_BY_SERUM_DEPRIVATION_UP, GRAESSMANN_RESPONSE_TO_MC_AND_SERUM_DEPRIVATION_UP, GOBP_REGULATION_OF_HORMONE_LEVELS

GO Biological Process (20): immune response (GO:0006955), cell surface receptor signaling pathway (GO:0007166), adenylate cyclase-activating G protein-coupled receptor signaling pathway (GO:0007189), activation of adenylate cyclase activity (GO:0007190), female pregnancy (GO:0007565), parturition (GO:0007567), adrenal gland development (GO:0030325), exploration behavior (GO:0035640), fear response (GO:0042596), behavioral response to ethanol (GO:0048149), corticotropin secretion (GO:0051458), general adaptation syndrome, behavioral process (GO:0051867), cellular response to corticotropin-releasing hormone stimulus (GO:0071376), negative regulation of voltage-gated calcium channel activity (GO:1901386), regulation of corticosterone secretion (GO:2000852), signal transduction (GO:0007165), G protein-coupled receptor signaling pathway (GO:0007186), hormone-mediated signaling pathway (GO:0009755), cellular response to hormone stimulus (GO:0032870), regulation of transport (GO:0051049)

GO Molecular Function (7): G protein-coupled receptor activity (GO:0004930), G protein-coupled peptide receptor activity (GO:0008528), corticotrophin-releasing factor receptor activity (GO:0015056), corticotropin-releasing hormone receptor activity (GO:0043404), corticotropin-releasing hormone binding (GO:0051424), transmembrane signaling receptor activity (GO:0004888), protein binding (GO:0005515)

GO Cellular Component (6): endosome (GO:0005768), plasma membrane (GO:0005886), membrane (GO:0016020), neuron projection (GO:0043005), postsynaptic density membrane (GO:0098839), glutamatergic synapse (GO:0098978)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
GPCR ligand binding	1
GPCR downstream signalling	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
signal transduction	3
G protein-coupled receptor activity	3
multi-organism reproductive process	2
multi-multicellular organism process	2
behavior	2
signaling receptor activity	2
immune system process	1
response to stimulus	1
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	1
adenylate cyclase activator activity	1
positive regulation of adenylate cyclase activity	1
endocrine system development	1
gland development	1
multicellular organismal response to stress	1
adult behavior	1
response to ethanol	1
peptide hormone secretion	1
general adaptation syndrome	1
response to corticotropin-releasing hormone	1
cellular response to peptide hormone stimulus	1
voltage-gated calcium channel activity	1
negative regulation of calcium ion transmembrane transporter activity	1
regulation of voltage-gated calcium channel activity	1
corticosterone secretion	1
regulation of glucocorticoid secretion	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
cellular response to hormone stimulus	1
response to hormone	1
cellular response to chemical stimulus	1
cellular response to endogenous stimulus	1
transport	1
regulation of localization	1
transmembrane signaling receptor activity	1
G protein-coupled receptor signaling pathway	1
peptide receptor activity	1
cellular response to corticotropin-releasing hormone stimulus	1

Protein interactions and networks

STRING

2526 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CRHR1	CRH	P06850	999
CRHR1	UCN	P55089	999
CRHR1	UCN3	Q969E3	990
CRHR1	CRHBP	P24387	983
CRHR1	UCN2	Q96RP3	976
CRHR1	POMC	P01189	925
CRHR1	AVPR1B	P47901	888
CRHR1	KANSL1	Q7Z3B3	858
CRHR1	NR3C1	P04150	843
CRHR1	STH	Q8IWL8	841
CRHR1	ARRB2	P32121	779
CRHR1	PDYN	P01213	766
CRHR1	HCRT	O43612	756
CRHR1	OPRM1	P35372	731
CRHR1	FKBP5	Q13451	724

IntAct

140 interactions, top by confidence:

A	B	Type	Score
CRHR1	CRH	psi-mi:“MI:0407”(direct interaction)	0.680
CRH	CRHR1	psi-mi:“MI:0407”(direct interaction)	0.680
SCRIB	CRHR1	psi-mi:“MI:0407”(direct interaction)	0.620
DLG1	CRHR1	psi-mi:“MI:0407”(direct interaction)	0.620
CRHR1	DLG1	psi-mi:“MI:0407”(direct interaction)	0.620
CRHR1	SCRIB	psi-mi:“MI:0407”(direct interaction)	0.620
CRH	CRH	psi-mi:“MI:0407”(direct interaction)	0.440
SRPK1	CRHR1	psi-mi:“MI:0217”(phosphorylation reaction)	0.440
CRHR1	PDZK1	psi-mi:“MI:0407”(direct interaction)	0.440
CRHR1	MAST2	psi-mi:“MI:0407”(direct interaction)	0.440
CRHR1	SYNJ2BP	psi-mi:“MI:0407”(direct interaction)	0.440
CRHR1	MAGI1	psi-mi:“MI:0407”(direct interaction)	0.440
CRHR1	MAGI2	psi-mi:“MI:0407”(direct interaction)	0.440
CRHR1	MAGI3	psi-mi:“MI:0407”(direct interaction)	0.440
CRHR1	ARHGEF11	psi-mi:“MI:0407”(direct interaction)	0.440
CRHR1	DLG4	psi-mi:“MI:0407”(direct interaction)	0.440
CRHR1	SNX27	psi-mi:“MI:0407”(direct interaction)	0.440
CRHR1	MAST1	psi-mi:“MI:0407”(direct interaction)	0.440
CRHR1	TAMALIN	psi-mi:“MI:0407”(direct interaction)	0.440
CRHR1	DLG2	psi-mi:“MI:0407”(direct interaction)	0.440
CRHR1	ARHGEF12	psi-mi:“MI:0407”(direct interaction)	0.440
CRHR1	DLG3	psi-mi:“MI:0407”(direct interaction)	0.440
CRHR1	PTPN3	psi-mi:“MI:0407”(direct interaction)	0.440

BioGRID (29): CRH (Protein-peptide), Dlg1 (Affinity Capture-Western), CRHR1 (Reconstituted Complex), CRHR1 (Reconstituted Complex), CRHR1 (Reconstituted Complex), CRHR1 (Reconstituted Complex), CRHR1 (Reconstituted Complex), CRHR1 (Reconstituted Complex), CRHR1 (Reconstituted Complex), CRHR1 (Reconstituted Complex), CRHR1 (Reconstituted Complex), DLG1 (Affinity Capture-Western), DLG4 (Affinity Capture-Western), UCN (Reconstituted Complex), CRHR1 (Reconstituted Complex)

ESM2 similar proteins: A0A324, B0BM39, B3VSC2, F6RQL9, O14817, O42602, O43688, O62772, O75954, O89035, P10063, P23576, P26048, P27681, P28473, P34998, P35347, P35353, P47869, P56880, Q05B83, Q06AA5, Q0VC00, Q13126, Q3SYV5, Q4L208, Q5R6I6, Q5RAP3, Q5RCC5, Q5ZJ75, Q6DCQ3, Q6GMK6, Q76LL8, Q86UF1, Q8BJU2, Q8BZH0, Q8JFQ2, Q8R3S2, Q8R4D1, Q8WU67

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

18 interactions.

A	Effect	B	Mechanism
CRH	up-regulates	CRHR1	binding
“GABA-A (a1-b1-g2) receptor”	down-regulates	CRHR1
“GABA-A (a2-b1-g2) receptor”	down-regulates	CRHR1
“GABA-A (a3-b1-g2) receptor”	down-regulates	CRHR1
“GABA-A (a4-b1-g2) receptor”	down-regulates	CRHR1
“GABA-A (a4-b2-d) receptor”	down-regulates	CRHR1
“GABA-A (a4-b3-d) receptor”	down-regulates	CRHR1
“GABA-A (a5-b1-g2) receptor”	down-regulates	CRHR1
“GABA-A (a6-b1-g2) receptor”	down-regulates	CRHR1
“GABA-A (a6-b2-d) receptor”	down-regulates	CRHR1
“GABA-A (a6-b3-d) receptor”	down-regulates	CRHR1
GABA-A	down-regulates	CRHR1
CRHR1	“up-regulates quantity by expression”	POMC	“transcriptional regulation”
CRHR1	“up-regulates quantity by expression”	Corticotropin	“transcriptional regulation”
CRHR1	“up-regulates quantity by expression”	Beta-endorphin	“transcriptional regulation”
CRHR1	“up-regulates activity”	GNAS	binding
CRHR1	“up-regulates activity”	GNAI1	binding
CRHR1	“up-regulates activity”	GNAQ	binding

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 84 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:

Pathway	Partners	Fold	FDR
Ras activation upon Ca2+ influx through NMDA receptor	5	51.9×	2e-06
Unblocking of NMDA receptors, glutamate binding and activation	5	49.4×	2e-06
Negative regulation of NMDA receptor-mediated neuronal transmission	5	49.4×	2e-06
Dopamine Neurotransmitter Release Cycle	5	45.1×	3e-06
Long-term potentiation	5	43.3×	3e-06
Assembly and cell surface presentation of NMDA receptors	9	41.5×	9e-11
Neurexins and neuroligins	11	39.4×	7e-13
Protein-protein interactions at synapses	7	33.8×	1e-07

GO biological processes:

GO term	Partners	Fold	FDR
establishment or maintenance of epithelial cell apical/basal polarity	9	66.2×	4e-12
protein localization to synapse	6	58.2×	2e-07
receptor clustering	6	47.4×	4e-07
regulation of postsynaptic membrane neurotransmitter receptor levels	6	37.6×	1e-06
bicellular tight junction assembly	5	20.9×	2e-04
protein-containing complex assembly	8	11.5×	4e-05
protein localization to plasma membrane	8	11.0×	5e-05
cell-cell adhesion	8	10.3×	7e-05

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	32
Likely pathogenic	4
Uncertain significance	49
Likely benign	8
Benign	6

Top pathogenic / likely-pathogenic (30)

Variant ID	HGVS	Classification
144496	GRCh38/hg38 17q21.31(chr17:45578381-46130670)x1	Pathogenic
145067	GRCh38/hg38 17q21.31(chr17:45629520-46130611)x1	Pathogenic
147646	GRCh38/hg38 17q21.31(chr17:45640337-46267672)x1	Pathogenic
148313	GRCh38/hg38 17q21.31(chr17:45574365-46273786)x1	Pathogenic
148451	GRCh38/hg38 17q21.31(chr17:45629520-46273786)x1	Pathogenic
148938	GRCh38/hg38 17q21.31(chr17:45629520-46094581)x1	Pathogenic
148960	GRCh38/hg38 17q21.31(chr17:45516110-46211895)x1	Pathogenic
150548	GRCh38/hg38 17q21.31(chr17:45579327-46130578)x1	Pathogenic
153206	GRCh38/hg38 17q21.31(chr17:45544831-46124104)x1	Pathogenic
155320	GRCh38/hg38 17q21.31(chr17:45626435-46110126)x1	Pathogenic
160838	GRCh38/hg38 17q21.31(chr17:45578381-46273786)x1	Pathogenic
161014	GRCh38/hg38 17q21.31(chr17:45629520-46111134)x1	Pathogenic
1703537	GRCh37/hg19 17q21.31(chr17:43703801-44212416)	Pathogenic
1710919	GRCh37/hg19 17q21.31(chr17:43703801-44212416)x1	Pathogenic
1808674	GRCh37/hg19 17q21.31(chr17:43622197-44212416)x1	Pathogenic
253584	GRCh37/hg19 17q21.31(chr17:43592410-44249054)x1	Pathogenic
32010	GRCh38/hg38 17q21.31(chr17:45629520-46111134)x1	Pathogenic
35239	GRCh38/hg38 17q21.31(chr17:45578381-46273786)x1	Pathogenic
394430	GRCh37/hg19 17q21.31(chr17:43585760-44248995)x1	Pathogenic
395154	GRCh37/hg19 17q21.31(chr17:43708346-44158662)x3	Pathogenic
442059	GRCh37/hg19 17q21.31(chr17:43710370-44212416)x1	Pathogenic
442854	GRCh37/hg19 17q21.31(chr17:43703800-44212416)x1	Pathogenic
443423	GRCh37/hg19 17q21.31(chr17:43703801-44212416)x1	Pathogenic
57279	GRCh38/hg38 17q21.31(chr17:45629520-46061206)x1	Pathogenic
57290	GRCh38/hg38 17q21.31(chr17:45578381-46111134)x1	Pathogenic
57525	GRCh38/hg38 17q21.31(chr17:45598042-46273786)x1	Pathogenic
57528	GRCh38/hg38 17q21.31(chr17:45629520-46051878)x1	Pathogenic
57539	GRCh38/hg38 17q21.31(chr17:45637714-46118962)x1	Pathogenic
57540	GRCh38/hg38 17q21.31(chr17:45640337-46273786)x1	Pathogenic
57541	GRCh38/hg38 17q21.31(chr17:45674308-46273786)x1	Pathogenic

SpliceAI

2224 predictions. Top by Δscore:

Variant	Effect	Δscore
17:45807098:G:A	donor_loss	1.0000
17:45807099:T:A	donor_loss	1.0000
17:45816583:G:GG	donor_gain	1.0000
17:45816588:G:GT	donor_gain	1.0000
17:45821438:G:GT	donor_gain	1.0000
17:45829213:A:AG	acceptor_gain	1.0000
17:45829214:G:GG	acceptor_gain	1.0000
17:45829317:CTCAG:C	donor_loss	1.0000
17:45829318:TCAG:T	donor_loss	1.0000
17:45829319:CAGGT:C	donor_loss	1.0000
17:45829320:AGGTG:A	donor_loss	1.0000
17:45829321:GG:G	donor_loss	1.0000
17:45829323:T:A	donor_loss	1.0000
17:45830059:A:AG	acceptor_gain	1.0000
17:45830059:ATC:A	acceptor_gain	1.0000
17:45830060:T:G	acceptor_gain	1.0000
17:45830061:C:A	acceptor_gain	1.0000
17:45830068:A:AG	acceptor_gain	1.0000
17:45830069:T:G	acceptor_gain	1.0000
17:45830071:A:AG	acceptor_gain	1.0000
17:45830072:T:G	acceptor_gain	1.0000
17:45830075:A:AG	acceptor_gain	1.0000
17:45830075:ACCC:A	acceptor_gain	1.0000
17:45830076:C:G	acceptor_gain	1.0000
17:45830078:C:CA	acceptor_gain	1.0000
17:45830083:T:TA	acceptor_gain	1.0000
17:45830086:T:A	acceptor_gain	1.0000
17:45830089:A:AG	acceptor_gain	1.0000
17:45830089:ACCAG:A	acceptor_gain	1.0000
17:45830090:C:G	acceptor_gain	1.0000

AlphaMissense

2720 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
17:45816506:G:C	W55C	1.000
17:45816506:G:T	W55C	1.000
17:45821367:G:C	R85P	1.000
17:45821372:T:A	C87S	1.000
17:45821373:G:C	C87S	1.000
17:45821392:G:C	W93C	1.000
17:45821392:G:T	W93C	1.000
17:45821417:T:A	C102S	1.000
17:45821418:G:C	C102S	1.000
17:45830132:T:C	L187P	1.000
17:45830499:T:C	L242P	1.000
17:45830906:T:A	W275R	1.000
17:45830906:T:C	W275R	1.000
17:45833457:T:A	N312K	1.000
17:45833457:T:G	N312K	1.000
17:45833489:T:C	L323P	1.000
17:45833746:C:G	P350R	1.000
17:45833754:G:C	G353R	1.000
17:45816471:T:A	C44S	0.999
17:45816472:G:C	C44S	0.999
17:45816504:T:A	W55R	0.999
17:45816504:T:C	W55R	0.999
17:45816543:T:A	C68S	0.999
17:45816544:G:A	C68Y	0.999
17:45816544:G:C	C68S	0.999
17:45821372:T:C	C87R	0.999
17:45821374:C:G	C87W	0.999
17:45821390:T:A	W93R	0.999
17:45821390:T:C	W93R	0.999
17:45821417:T:C	C102R	0.999

dbSNP variants (sampled 300 via entrez): RS1000047582 (17:45786132 T>TC,TG), RS1000089367 (17:45817164 G>A), RS1000114237 (17:45797520 C>T), RS1000169438 (17:45828327 G>A), RS1000182987 (17:45830566 C>G,T), RS1000195175 (17:45802559 A>G), RS1000249614 (17:45782736 C>A), RS1000269875 (17:45822636 A>C), RS1000289963 (17:45833907 G>A,T), RS1000347607 (17:45795124 G>A), RS1000367256 (17:45796996 G>T), RS1000379107 (17:45785916 GA>G), RS1000401147 (17:45788941 C>T), RS1000499541 (17:45801182 C>A,G,T), RS1000658366 (17:45801464 G>A)

Disease associations

OMIM: gene MIM:122561 | disease phenotypes: MIM:610443

GenCC curated gene-disease

Mondo (2): Koolen-de Vries syndrome (MONDO:0012496), frontotemporal dementia (MONDO:0017276)

Orphanet (2): Koolen-De Vries syndrome (Orphanet:96169), Frontotemporal dementia (Orphanet:282)

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

66 associations (top):

Study	Trait	p-value
GCST000494_7	Bone mineral density (spine)	1.000000e-08
GCST000495_9	Bone mineral density (hip)	4.000000e-06
GCST001483_2	Intracranial volume	8.000000e-15
GCST001484_2	Head circumference (infant)	4.000000e-06
GCST001974_3	Idiopathic pulmonary fibrosis	6.000000e-09
GCST002756_10	Subcortical brain region volumes	1.000000e-08
GCST002756_8	Subcortical brain region volumes	8.000000e-09
GCST002817_26	Alzheimer’s disease in APOE e4- carriers	5.000000e-06
GCST003784_19	Multiple system atrophy	7.000000e-07
GCST003984_2	Parkinson’s disease	4.000000e-32
GCST003996_26	Monobrow	3.000000e-32
GCST003998_7	Joint mobility (Beighton score)	6.000000e-11
GCST004604_30	Hematocrit	2.000000e-28
GCST004613_67	Sum neutrophil eosinophil counts	6.000000e-09
GCST004614_63	Granulocyte count	5.000000e-09
GCST004615_112	Hemoglobin concentration	3.000000e-26
GCST004620_31	Sum basophil neutrophil counts	2.000000e-11
GCST004626_146	Myeloid white cell count	3.000000e-09
GCST004629_32	Neutrophil count	3.000000e-11
GCST004902_11	Parkinson’s disease	1.000000e-68
GCST005232_131	Neuroticism	8.000000e-26
GCST005337_5	Headache	6.000000e-15
GCST005581_16	Primary biliary cirrhosis	2.000000e-09
GCST006099_2	Accelerometer-based physical activity measurement (average acceleration)	5.000000e-12
GCST006481_28	Lung function (FEV1)	3.000000e-10
GCST006481_32	Lung function (FEV1)	1.000000e-09
GCST006481_9	Lung function (FEV1)	9.000000e-10
GCST006483_24	Lung function (FVC)	2.000000e-09
GCST006483_25	Lung function (FVC)	2.000000e-07
GCST006661_281	Male-pattern baldness	8.000000e-29

EFO canonical traits (30, from GWAS)

EFO ID	Trait name
EFO:0004886	intracranial volume measurement
EFO:0000768	idiopathic pulmonary fibrosis
EFO:0007906	synophrys measurement
EFO:0007905	joint hypermobility measurement
EFO:0004348	hematocrit
EFO:0004833	neutrophil count
EFO:0004842	eosinophil count
EFO:0007987	granulocyte count
EFO:0004509	hemoglobin measurement
EFO:0005090	basophil count
EFO:0007660	neuroticism measurement
EFO:0008002	physical activity measurement
EFO:0004314	forced expiratory volume
EFO:0004312	vital capacity
EFO:0009458	alcohol use disorder measurement
EFO:0009925	Antithrombotic agent use measurement
EFO:0008475	mood instability measurement
EFO:0010158	sugar consumption measurement
EFO:0008320	white matter volume measurement
EFO:0009695	household income
EFO:0008381	total cortical area measurement
EFO:0004346	neuroimaging measurement
EFO:0007828	daytime rest measurement
EFO:0007991	eosinophil percentage of leukocytes
EFO:0004587	lymphocyte count
EFO:0007986	reticulocyte count
EFO:0009902	handedness
EFO:0007789	BMI-adjusted waist circumference
EFO:0007788	BMI-adjusted waist-hip ratio
EFO:0008039	BMI-adjusted hip circumference

MeSH disease descriptors (1)

Descriptor	Name	Tree numbers
D057180	Frontotemporal Dementia	C10.228.140.380.266.299; C10.574.950.300.299; C18.452.845.800.300.299; F03.615.400.380.299

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL1800 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

6 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 16,659 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL291657	CRINECERFONT	4	140
CHEMBL286494	HYPERICIN	3	16,266
CHEMBL482950	PEXACERFONT	3	91
CHEMBL1287935	VERUCERFONT	2	80
CHEMBL1819077	ONO-2333MS	2	39
CHEMBL514270	EMICERFONT	2	43

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

PharmGKB clinical annotations

3 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs1876828	Efficacy	3	corticosteroids	Asthma
rs242941	Efficacy	3	fluoxetine	Anxiety Disorders;Major Depressive Disorder
rs28364032	Efficacy	3	antidepressants	Major Depressive Disorder

PharmGKB variants

30 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs110402	CRHR1		0.00	0
rs242939	CRHR1		0.00	0
rs242941	CRHR1	3	1.75	1	fluoxetine
rs739645	CRHR1		0.00	0
rs1876828	CRHR1	3	3.50	1	corticosteroids
rs1876829	CRHR1		0.00	0
rs1876831	CRHR1		0.00	0
rs28364032	CRHR1	3	3.25	1	antidepressants
rs9892359	CRHR1		0.00	0
rs4792886	CRHR1		0.00	0
rs4792887	CRHR1		0.00	0
rs12103667	CRHR1		0.00	0
rs3785877	CRHR1		0.00	0
rs171440	CRHR1		0.00	0
rs16940655	CRHR1		0.00	0
rs12150390	CRHR1		0.00	0
rs242936	CRHR1		0.00	0
rs1912151	CRHR1		0.00	0
rs1396862	CRHR1		0.00	0
rs17763086	CRHR1		0.00	0
rs75638861	CRHR1		0.00	0
rs16940665	CRHR1		0.00	0
rs17689966	CRHR1		0.00	0
rs16940674	CRHR1		0.00	0
rs878886	CRHR1		0.00	0
rs878887	CRHR1		0.00	0
rs878888	CRHR1		0.00	0
rs4525537	CRHR1		0.00	0
rs4640231	CRHR1		0.00	0
rs16940686	CRHR1		0.00	0

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Corticotropin-releasing factor receptors

Most potent curated ligand interactions (30 total), top 25:

Ligand	Action	Affinity	Parameter
CP 154,526	Antagonist	10.41	pIC50
[125I]sauvagine (frog)	Full agonist	10.0	pKd
[125I]urocortin 1 (mouse, rat)	Full agonist	10.0	pKd
urocortin 1	Full agonist	9.8	pKd
[125I]CRF (ovine)	Full agonist	9.5	pKd
urocortin 1	Full agonist	9.5	pKd
urotensin 1 (fish)	Full agonist	9.4	pKd
[125I]Tyr0-CRF (human, rat, mouse)	Full agonist	9.3	pKd
[125I]astressin	Antagonist	9.3	pKd
sauvagine	Full agonist	9.2	pKd
antalarmin	Antagonist	9.0	pKi
DMP696	Antagonist	9.0	pKi
NBI27914	Antagonist	9.0	pKi
R121919	Antagonist	9.0	pKi
corticotrophin-releasing hormone	Full agonist	9.0	pKd
corticotropin-releasing factor	Full agonist	8.9	pKd
crinecerfont	Antagonist	8.7	pKi
astressin	Antagonist	8.7	pKi
ONO-2333MS	Antagonist	8.4	pIC50
NBI-35965	Antagonist	8.4	pKi
tildacerfont	Antagonist	8.3	pKi
CP 376,395	Antagonist	8.3	pIC50
NBI-34041	Antagonist	8.29	pKi
verucerfont	Antagonist	8.2	pKi
CP-316,311	Antagonist	8.07	pKi

Binding affinities (BindingDB)

200 measured of 200 human assays (200 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
CP 154,526	KI	0.4 nM
DMP904	KI	0.4 nM
NSC_0	KI	1.4 nM
DMP696	KI	1.8 nM
CAS_197801-88-0	KI	4.9 nM
2-chloro-N-[4-[(3-ethyl-5-methylpyrazol-1-yl)methyl]cyclohexyl]-5-(trifluoromethyl)benzamide	IC50	13 nM	US-8835444: Cyclohexyl amide derivatives as CRF receptor antagonists
2-chloro-N-[4-[[(5-fluoro-4-methyl-2-pyridinyl)amino]methyl]cyclohexyl]-5-(trifluoromethyl)benzamide	IC50	13 nM	US-8614213: Cyclohexyl amide derivatives and their use as CRF-1 receptor antagonists
2-chloro-N-[4-[[[4-(4-chlorophenyl)-1H-pyrazol-5-yl]amino]methyl]cyclohexyl]-5-(trifluoromethyl)benzamide	IC50	15 nM	US-8614213: Cyclohexyl amide derivatives and their use as CRF-1 receptor antagonists
2-chloro-N-[4-[[(4-fluoro-1H-indazol-3-yl)amino]methyl]cyclohexyl]-5-(trifluoromethyl)benzamide	IC50	17 nM	US-8614213: Cyclohexyl amide derivatives and their use as CRF-1 receptor antagonists
N-cyclopentyl-3-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-6-methoxy-N-(2-methoxyethyl)pyrazolo[5,1-b][1,3]thiazol-7-amine	IC50	18 nM	US-8530504: Pyrazolothiazole compound
3-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-6-methoxy-N-(2-methoxyethyl)-N-(2-methylpropyl)pyrazolo[5,1-b][1,3]thiazol-7-amine	IC50	19 nM	US-8530504: Pyrazolothiazole compound
2-chloro-N-[4-[[(2-methyl-3-pyridinyl)amino]methyl]cyclohexyl]-5-(trifluoromethyl)benzamide	IC50	19 nM	US-8614213: Cyclohexyl amide derivatives and their use as CRF-1 receptor antagonists
2-chloro-N-[4-[[(5-chloro-2-methyl-3-pyridinyl)amino]methyl]cyclohexyl]-5-(trifluoromethyl)benzamide	IC50	19 nM	US-8614213: Cyclohexyl amide derivatives and their use as CRF-1 receptor antagonists
N-cyclohexyl-3-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-6-methoxy-N-(2-methoxyethyl)pyrazolo[5,1-b][1,3]thiazol-7-amine	IC50	20 nM	US-8530504: Pyrazolothiazole compound
2-chloro-N-[4-[(3,5-diethylpyrazol-1-yl)methyl]cyclohexyl]-5-(trifluoromethyl)benzamide	IC50	21 nM	US-8835444: Cyclohexyl amide derivatives as CRF receptor antagonists
2-chloro-N-[4-[(5-ethyl-3-methylpyrazol-1-yl)methyl]cyclohexyl]-5-(trifluoromethyl)benzamide	IC50	22 nM	US-8835444: Cyclohexyl amide derivatives as CRF receptor antagonists
2-chloro-N-[4-[(3,5-dimethylpyrazol-1-yl)methyl]cyclohexyl]-5-(trifluoromethyl)benzamide	IC50	22 nM	US-8614213: Cyclohexyl amide derivatives and their use as CRF-1 receptor antagonists
2-chloro-N-[4-[[(5-chloro-4-methyl-2-pyridinyl)amino]methyl]cyclohexyl]-5-(trifluoromethyl)benzamide	IC50	22 nM	US-8614213: Cyclohexyl amide derivatives and their use as CRF-1 receptor antagonists
2-chloro-N-[4-[[(5-fluoro-2-pyridinyl)amino]methyl]cyclohexyl]-5-(trifluoromethyl)benzamide	IC50	23 nM	US-8614213: Cyclohexyl amide derivatives and their use as CRF-1 receptor antagonists
NSC_0	KI	23.1 nM
N-cyclobutyl-3-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-N-ethyl-6-methoxypyrazolo[5,1-b][1,3]thiazol-7-amine	IC50	24 nM	US-8530504: Pyrazolothiazole compound
N-butyl-3-[4-(ethoxymethyl)-2,6-dimethoxyphenyl]-6-methoxy-N-(2-methoxyethyl)pyrazolo[5,1-b][1,3]thiazol-7-amine	IC50	25 nM	US-8530504: Pyrazolothiazole compound
N-(cyclobutylmethyl)-3-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-6-methoxy-N-(2-methoxyethyl)pyrazolo[5,1-b][1,3]thiazol-7-amine	IC50	25 nM	US-8530504: Pyrazolothiazole compound
3-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-6-methoxy-N,N-dipropylpyrazolo[5,1-b][1,3]thiazol-7-amine	IC50	26 nM	US-8530504: Pyrazolothiazole compound
3-[4-(ethoxymethyl)-2,6-dimethoxyphenyl]-6-methoxy-N-(oxolan-3-yl)-N-propylpyrazolo[5,1-b][1,3]thiazol-7-amine	IC50	26 nM	US-8530504: Pyrazolothiazole compound
N-cyclopentyl-3-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-N-ethyl-6-methoxypyrazolo[5,1-b][1,3]thiazol-7-amine	IC50	26 nM	US-8530504: Pyrazolothiazole compound
2-chloro-N-[4-[[(5-fluoro-3-pyridinyl)amino]methyl]cyclohexyl]-5-(trifluoromethyl)benzamide	IC50	26 nM	US-8614213: Cyclohexyl amide derivatives and their use as CRF-1 receptor antagonists
2-chloro-N-[4-[[(5-ethyl-3-pyridinyl)amino]methyl]cyclohexyl]-5-(trifluoromethyl)benzamide	IC50	28 nM	US-8614213: Cyclohexyl amide derivatives and their use as CRF-1 receptor antagonists
2-chloro-N-[4-[[(1-methylindazol-3-yl)amino]methyl]cyclohexyl]-5-(trifluoromethyl)benzamide	IC50	29 nM	US-8614213: Cyclohexyl amide derivatives and their use as CRF-1 receptor antagonists
2-chloro-N-[4-[[(1-phenyltetrazol-5-yl)amino]methyl]cyclohexyl]-5-(trifluoromethyl)benzamide	IC50	29 nM	US-8614213: Cyclohexyl amide derivatives and their use as CRF-1 receptor antagonists
N-cyclobutyl-3-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-6-methoxy-N-(2-methoxyethyl)pyrazolo[5,1-b][1,3]thiazol-7-amine	IC50	31 nM	US-8530504: Pyrazolothiazole compound
2,5-dichloro-N-[4-[[(4,5-dimethyl-1,3-thiazol-2-yl)amino]methyl]cyclohexyl]pyridine-3-carboxamide	IC50	31 nM	US-8614213: Cyclohexyl amide derivatives and their use as CRF-1 receptor antagonists
2-chloro-N-[4-[(4,5,6,7-tetrahydro-1H-indazol-3-ylamino)methyl]cyclohexyl]-5-(trifluoromethyl)benzamide	IC50	31 nM	US-8614213: Cyclohexyl amide derivatives and their use as CRF-1 receptor antagonists
N-(cyclopropylmethyl)-3-[4-(ethoxymethyl)-2,6-dimethoxyphenyl]-6-methoxy-N-(2-methoxyethyl)pyrazolo[5,1-b][1,3]thiazol-7-amine	IC50	32 nM	US-8530504: Pyrazolothiazole compound
N-(cyclobutylmethyl)-3-[4-(ethoxymethyl)-2,6-dimethoxyphenyl]-6-methoxy-N-(oxolan-3-yl)pyrazolo[5,1-b][1,3]thiazol-7-amine	IC50	32 nM	US-8530504: Pyrazolothiazole compound
2-chloro-N-[4-[[(6-methoxy-1H-indazol-3-yl)amino]methyl]cyclohexyl]-5-(trifluoromethyl)benzamide	IC50	32 nM	US-8614213: Cyclohexyl amide derivatives and their use as CRF-1 receptor antagonists
N-(cyclopropylmethyl)-3-(2,6-dimethoxy-4-methylphenyl)-6-methoxy-N-(oxolan-3-ylmethyl)pyrazolo[5,1-b][1,3]thiazol-7-amine	IC50	33 nM	US-8530504: Pyrazolothiazole compound
3-(4-cyclopropyl-2,6-dimethoxyphenyl)-N-(cyclopropylmethyl)-6-methoxy-N-(oxolan-3-ylmethyl)pyrazolo[5,1-b][1,3]thiazol-7-amine	IC50	33 nM	US-8530504: Pyrazolothiazole compound
3-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-6-methoxy-N-propyl-N-pyridin-2-ylpyrazolo[5,1-b][1,3]thiazol-7-amine	IC50	33 nM	US-8530504: Pyrazolothiazole compound
1-(4-{3-[4-(6-Fluoro-benzo[d]isoxazol-3-yl)-piperidin-1-yl]-propoxy}-3-methoxy-phenyl)-ethanone	KI	33 nM
2-chloro-N-[4-[[(4-chloro-5-methyl-1H-pyrazol-3-yl)amino]methyl]cyclohexyl]-5-(trifluoromethyl)benzamide	IC50	34 nM	US-8614213: Cyclohexyl amide derivatives and their use as CRF-1 receptor antagonists
N-(cyclopropylmethyl)-3-[4-(ethoxymethyl)-2,6-dimethoxyphenyl]-6-methoxy-N-(3-methoxypropyl)pyrazolo[5,1-b][1,3]thiazol-7-amine	IC50	35 nM	US-8530504: Pyrazolothiazole compound
2-chloro-N-[4-[[[4-(2-chloro-4-methoxyphenyl)-5-methylpyrazolidin-3-yl]amino]methyl]cyclohexyl]-5-(trifluoromethyl)benzamide	IC50	35 nM	US-8835444: Cyclohexyl amide derivatives as CRF receptor antagonists
N-(cyclopropylmethyl)-3-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-6-methoxy-N-(2-methoxypropyl)pyrazolo[5,1-b][1,3]thiazol-7-amine	IC50	36 nM	US-8530504: Pyrazolothiazole compound
3-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-6-methoxy-N-propyl-N-pyridin-3-ylpyrazolo[5,1-b][1,3]thiazol-7-amine	IC50	36 nM	US-8530504: Pyrazolothiazole compound
2-chloro-N-[4-[[(5-methyl-1,3-thiazol-2-yl)amino]methyl]cyclohexyl]-5-(trifluoromethyl)benzamide	IC50	36 nM	US-8614213: Cyclohexyl amide derivatives and their use as CRF-1 receptor antagonists
2-chloro-N-[4-[[(4-methyl-5-phenyl-1H-pyrazol-3-yl)amino]methyl]cyclohexyl]-5-(trifluoromethyl)benzamide	IC50	37 nM	US-8614213: Cyclohexyl amide derivatives and their use as CRF-1 receptor antagonists
2-chloro-N-[4-[[(4-pyridin-3-yl-1H-pyrazol-5-yl)amino]methyl]cyclohexyl]-5-(trifluoromethyl)benzamide	IC50	37 nM	US-8614213: Cyclohexyl amide derivatives and their use as CRF-1 receptor antagonists
N-[3-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-2-ethyl-6-methoxypyrazolo[5,1-b][1,3]thiazol-7-yl]-1-hydroxycyclopropane-1-carboxamide	IC50	37 nM	US-8530504: Pyrazolothiazole compound
2-chloro-N-[4-[[(3-methyl-2-pyridinyl)amino]methyl]cyclohexyl]-5-(trifluoromethyl)benzamide	IC50	38 nM	US-8614213: Cyclohexyl amide derivatives and their use as CRF-1 receptor antagonists

ChEMBL bioactivities

2301 potent at pChembl≥5 of 2313 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.80	Ki	0.16	nM	CHEMBL4299295
9.74	Ki	0.18	nM	CHEMBL3775796
9.70	Ki	0.2	nM	CHEMBL4299341
9.70	Ki	0.2	nM	CHEMBL3774395
9.70	Ki	0.2	nM	CHEMBL498311
9.66	EC50	0.22	nM	CHEMBL427807
9.66	Ki	0.22	nM	CHEMBL3774868
9.62	Ki	0.24	nM	CHEMBL3775030
9.62	IC50	0.24	nM	CHEMBL2370939
9.60	Ki	0.25	nM	CHEMBL3774682
9.55	Ki	0.28	nM	CHEMBL3774395
9.55	Kd	0.279	nM	CHEMBL45187
9.54	Ki	0.29	nM	CHEMBL4299349
9.54	Ki	0.291	nM	CHEMBL1836947
9.54	Kd	0.291	nM	CHEMBL1836947
9.52	Ki	0.3	nM	CHEMBL4299348
9.52	Kd	0.303	nM	CHEMBL309138
9.52	EC50	0.3	nM	CHEMBL1939594
9.51	Ki	0.31	nM	CHEMBL3775796
9.47	Ki	0.34	nM	CHEMBL3775621
9.46	Ki	0.35	nM	CHEMBL4299340
9.43	Ki	0.373	nM	CHEMBL1836945
9.43	Kd	0.373	nM	CHEMBL1836945
9.40	Ki	0.4	nM	CHEMBL341820
9.38	Ki	0.42	nM	CHEMBL3775678
9.37	Ki	0.43	nM	CHEMBL3775778
9.35	Ki	0.45	nM	CHEMBL4299352
9.34	Ki	0.46	nM	CHEMBL4299286
9.32	Ki	0.48	nM	CHEMBL4299295
9.31	Ki	0.49	nM	CHEMBL3775437
9.31	Ki	0.49	nM	CHEMBL3775812
9.30	Ki	0.5	nM	CHEMBL3774594
9.30	Ki	0.5	nM	CHEMBL115389
9.28	Ki	0.52	nM	CHEMBL3775761
9.28	Ki	0.53	nM	CHEMBL4299308
9.23	Ki	0.59	nM	CHEMBL3775192
9.22	Ki	0.6	nM	CHEMBL344223
9.22	EC50	0.6	nM	CHEMBL1939601
9.21	Ki	0.62	nM	CHEMBL115142
9.21	Ki	0.61	nM	CHEMBL3774939
9.19	Ki	0.64	nM	CHEMBL3775761
9.17	Ki	0.68	nM	CHEMBL3774836
9.17	Ki	0.68	nM	CHEMBL3775192
9.16	Ki	0.69	nM	CHEMBL3774485
9.16	Ki	0.69	nM	CHEMBL3774742
9.15	Ki	0.7	nM	CHEMBL4299297
9.15	Ki	0.7	nM	CHEMBL140894
9.15	EC50	0.7	nM	CHEMBL1830523
9.15	EC50	0.7	nM	CHEMBL1939583
9.14	Ki	0.73	nM	CHEMBL333735

PubChem BioAssay actives

4124 with measured affinity, of 5331 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.

Compound	Assay	Type	Value	Unit
4-[4-chloro-5-(2,6-dimethyl-8-pentan-3-ylimidazo[1,2-b]pyridazin-3-yl)-1,3-thiazol-2-yl]morpholine	362068: Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells	ki	0.0002	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-acetamido-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(3R,6S,9S,18S)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3-[[4-(carbamoylamino)phenyl]methyl]-6-methyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-oxopentanoic acid	1283233: Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0002	uM
(4S)-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(6S,9S,18S)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2-methyl-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3,3,6-trimethyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2-methyl-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-3-carboxy-2-(hexanoylamino)propanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]pentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]pentanoyl]amino]propanoyl]amino]-5-oxopentanoic acid	1283233: Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0002	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-acetamido-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(3S,6S,9S,18S)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3-(1H-imidazol-5-ylmethyl)-6-methyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-oxopentanoic acid	1283206: Displacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0002	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-acetamido-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(3S,6S,9S,18S)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxo-3-thiophen-2-ylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3-(1H-imidazol-5-ylmethyl)-6-methyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-oxopentanoic acid	1283233: Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0002	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R,3S)-2-[[(2R)-2-[[(2R)-2-acetamido-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(6R,9R,18R)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3,3,6-trimethyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-oxopentanoic acid	1283233: Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0002	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R,3R)-2-[[(2R)-2-[[(2S)-2-acetamido-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(3R,6R,9R,18R)-18-[[(2R)-4-amino-1-[[(2R)-1-[[(2R)-6-amino-1-[[(2R)-1-[[1-[[(2R)-1-[[1-[[(2R,3R)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3-(1H-imidazol-5-ylmethyl)-6-methyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-5-oxopentanoic acid	1283233: Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0002	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-1-[(2S)-4-amino-2-[[(2S)-2-amino-3-carboxypropanoyl]amino]-4-oxobutanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-3-methylpentanoyl]amino]-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-hydroxybutanoyl]amino]-5-oxopentanoyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-4-carboxybutanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]propanoyl]amino]-5-[[(2S)-5-amino-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S,3S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-oxopentanoic acid	220021: Activity of peptidic agonists on corticotropin releasing factor receptor using agonist-stimulated adenylate cyclase assay	ec50	0.0002	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(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-acetamido-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-2,4-dimethylpentanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-6-aminohexanoyl]amino]hexanoyl]amino]-3-methylpentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-4-carboxybutanoyl]amino]-6-aminohexanoyl]amino]-5-amino-5-oxopentanoyl]amino]-4-carboxybutanoyl]amino]-6-aminohexanoyl]amino]-5-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(5S,8S,11R,14R)-5-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-8,11-dimethyl-3,7,10,13,17-pentaoxo-1,2,6,9,12-pentazacycloheptadec-14-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-oxopentanoic acid	53828: Inhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine	ic50	0.0002	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-acetamido-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(3S,6S,9S,18S)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3-(1H-imidazol-5-ylmethyl)-6-methyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-oxopentanoic acid	1283233: Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0003	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-acetamido-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(3S,6S,9S,18S)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxo-3-thiophen-3-ylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3-(1H-imidazol-5-ylmethyl)-6-methyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-oxopentanoic acid	1283233: Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0003	uM
(4R)-4-[[(2R)-2-[[(2R)-2-[[(2R)-2-[2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-acetamido-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-[[(2R)-5-amino-1-[[1-[[(2R)-1-[[(2R)-5-amino-1-[[(3R,6S,9S,18S)-18-[[(2R)-4-amino-1-[[(2R)-1-[[(2R)-6-amino-1-[[(2R)-1-[[1-[[(2R)-1-[[1-[[(2R,3R)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3,6-dimethyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-oxopentanoic acid	1283206: Displacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0003	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R,3S)-2-[[(2R)-2-[[(2R)-2-acetamido-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(6R,9R,18R)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3,6-dimethyl-3-(2-methylpropyl)-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-oxopentanoic acid	1283233: Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0003	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R,3S)-2-[[(2R)-2-[[(2R)-2-acetamido-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(3S,6R,9R,18R)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3,6-dimethyl-3-(2-methylpropyl)-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-oxopentanoic acid	1283233: Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0003	uM
N-(dicyclopropylmethyl)-9-[4-(difluoromethoxy)-2-methoxyphenyl]-2,8-dimethylpurin-6-amine	622045: Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation	ki	0.0003	uM
2-[6-(difluoromethoxy)-2-methyl-3-pyridinyl]-3,7-dimethyl-5-pentan-3-ylpyrrolo[2,1-f][1,2,4]triazin-4-one	641201: Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay	ec50	0.0003	uM
3-[6-(dimethylamino)-4-methyl-3-pyridinyl]-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine	622092: Binding affinity to recombinant human CRF1 receptor expressed in CHO cells	kd	0.0003	uM
3-(4-methoxy-2-methylphenyl)-2,5-dimethyl-N-pentan-3-ylpyrazolo[1,5-a]pyrimidin-7-amine	622092: Binding affinity to recombinant human CRF1 receptor expressed in CHO cells	kd	0.0003	uM
N-butyl-8-(2,4-dichlorophenyl)-N-ethyl-2,7-dimethylpyrazolo[1,5-a][1,3,5]triazin-4-amine	53832: Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1	ki	0.0004	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-acetamido-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(3S,6S,9S,18S)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2-methyl-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3-(1H-imidazol-5-ylmethyl)-6-methyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2-methyl-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-oxopentanoic acid	1283233: Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0004	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-acetamido-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(3S,6S,9S,18S)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3-(1H-imidazol-5-ylmethyl)-6-methyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-oxopentanoic acid	1283233: Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0004	uM
(4R)-4-[[(2R)-2-[[(2R)-2-[[(2R)-2-[2-[[(2S)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-acetamido-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-[[(2R)-5-amino-1-[[1-[[(2R)-1-[[(2R)-5-amino-1-[[(3S,6S,9S,18S)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3-(1H-imidazol-5-ylmethyl)-6-methyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-oxopentanoic acid	1283233: Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0004	uM
9-[2-chloro-4-(difluoromethoxy)phenyl]-N-(dicyclopropylmethyl)-2,8-dimethylpurin-6-amine	622045: Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation	ki	0.0004	uM
(4S)-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(6S,9S,18S)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2-methyl-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3,3,6-trimethyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2-methyl-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-3-carboxy-2-(decanoylamino)propanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]pentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]pentanoyl]amino]propanoyl]amino]-5-oxopentanoic acid	1283206: Displacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0005	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-acetamido-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(3S,6S,9S,18S)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-naphthalen-1-yl-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3-(1H-imidazol-5-ylmethyl)-6-methyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-oxopentanoic acid	1283233: Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0005	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-acetamido-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(6S,9S,18S)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2-methyl-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3,3,6-trimethyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2-methyl-1-oxo-3-phenylpropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-oxopentanoic acid	1283233: Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0005	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-acetamido-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(3S,6S,9S,18S)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-naphthalen-2-yl-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3-(1H-imidazol-5-ylmethyl)-6-methyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-oxopentanoic acid	1283233: Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0005	uM
(4R)-4-[[(2R)-2-[[(2R)-2-[[(2R)-2-[2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-acetamido-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-[[(2R)-5-amino-1-[[1-[[(2R)-1-[[(2R)-5-amino-1-[[(3S,6S,9S,18S)-18-[[(2R)-4-amino-1-[[(2R)-1-[[(2R)-6-amino-1-[[(2R)-1-[[1-[[(2R)-1-[[1-[[(2R,3R)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3,6-dimethyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-oxopentanoic acid	1283233: Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0005	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2R)-2-acetamido-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(6R,9R,18R)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2-methyl-1-oxo-3-phenylpropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3,3,6-trimethyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2-methyl-1-oxo-3-phenylpropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-oxopentanoic acid	1283206: Displacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0005	uM
N-(cyclopropylmethyl)-8-(2,4-dichlorophenyl)-2-methyl-N-propylquinolin-4-amine	53971: Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand	ki	0.0005	uM
8-(2,4-dichlorophenyl)-2,7-dimethyl-N,N-dipropylpyrazolo[1,5-a][1,3,5]triazin-4-amine	53832: Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1	ki	0.0006	uM
(4S)-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(6S,9S,18S)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2-methyl-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3,3,6-trimethyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2-methyl-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-3-carboxy-2-(pentanoylamino)propanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]pentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]pentanoyl]amino]propanoyl]amino]-5-oxopentanoic acid	1283206: Displacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0006	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-acetamido-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(6S,9S,18S)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2-methyl-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3,3,6-trimethyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2-methyl-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-oxopentanoic acid	1283233: Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0006	uM
2-(4-methoxy-2,6-dimethylphenyl)-3,7-dimethyl-5-pentan-3-ylpyrrolo[2,1-f][1,2,4]triazin-4-one	641201: Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay	ec50	0.0006	uM
N,N-dibutyl-3-(2,4-dichlorophenyl)-1,5-dimethylpyrazolo[4,3-b]pyridin-7-amine	53974: Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells	ki	0.0006	uM
N-(cyclopropylmethyl)-8-(2,4-dichlorophenyl)-2,7-dimethyl-N-propylpyrazolo[1,5-a][1,3,5]triazin-4-amine	53832: Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1	ki	0.0007	uM
N-(2-chloro-4-methoxyphenyl)-3-pentan-3-yl-1,3,8,12-tetrazatricyclo[7.3.0.02,6]dodeca-2(6),4,7,9,11-pentaen-7-amine	620306: Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay	ec50	0.0007	uM
(4S)-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(6S,9S,18S)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2-methyl-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3,3,6-trimethyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2-methyl-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-3-carboxy-2-(propanoylamino)propanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]pentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]pentanoyl]amino]propanoyl]amino]-5-oxopentanoic acid	1283233: Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0007	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-acetamido-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-1-[[(3S,6S,9S,18S)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3-(1H-imidazol-5-ylmethyl)-6-methyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-2,4-dimethyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-oxopentanoic acid	1283233: Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0007	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-acetamido-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(6S,9S,18S)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2,3-dimethyl-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3,3,6-trimethyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2,3-dimethyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-oxopentanoic acid	1283233: Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0007	uM
(4S)-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(6S,9S,18S)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2-methyl-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3,3,6-trimethyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2-methyl-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-(butanoylamino)-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-oxopentanoic acid	1283233: Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0007	uM
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R,3R)-2-[[(2R)-2-[[(2S)-2-acetamido-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]amino]-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(6S,9S,18S)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2,3-dimethyl-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3,3,6-trimethyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2-methyl-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-oxopentanoic acid	1283233: Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0007	uM
N-(cyclopropylmethyl)-3-(2,4-dichlorophenyl)-2-methyl-5-methylsulfanyl-N-propylpyrazolo[1,5-a]pyrimidin-7-amine	53958: Binding affinity to the cloned human corticotropin releasing factor receptor 1	ki	0.0007	uM
(4S)-5-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(3R,6S,9S,18R)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S,3R)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3-(1H-imidazol-4-ylmethyl)-6-methyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-phenylpropanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoyl]amino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]propanoyl]amino]-5-oxopentanoic acid	53828: Inhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine	ic50	0.0007	uM
2-(2-chloro-4-methoxyphenyl)-3-ethyl-7-methyl-5-pentan-3-ylpyrrolo[2,1-f][1,2,4]triazin-4-one	641201: Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay	ec50	0.0007	uM
3-(2,4-dibromophenyl)-N-heptan-4-yl-5-methyltriazolo[4,5-d]pyrimidin-7-amine	53968: Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells	ki	0.0008	uM
(4S)-5-[[(2S)-5-amino-1-[[1-[[(2S)-1-[[(2S)-5-amino-1-[[(6S,9S,18S)-18-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[1-[[(2S)-1-[[1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-2-methyl-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]carbamoyl]-3,3,6-trimethyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-2-methyl-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-carbamimidamido-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-3-carboxy-2-(tetradecanoylamino)propanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]pentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoylamino]propanoyl]amino]pentanoyl]amino]propanoyl]amino]-5-oxopentanoic acid	1283233: Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay	ki	0.0008	uM
N-butyl-N-ethyl-2,5,6-trimethyl-7-(2,4,6-trimethylphenyl)pyrrolo[2,3-d]pyrimidin-4-amine	53968: Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells	ki	0.0008	uM
(2S,3S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-carboxy-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-carboxy-2-[[(2S,3S)-2-[[(2S)-3-hydroxy-2-[[(2S,3S)-3-methyl-2-[[(2S)-1-[(2S)-1-[2-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]acetyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]pentanoyl]amino]propanoyl]amino]-3-methylpentanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-4-methylpentanoyl]amino]butanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-methylpentanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-4-carboxybutanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-4-carboxybutanoyl]amino]hexanoyl]amino]-4-carboxybutanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]propanoyl]amino]-4-oxobutanoyl]amino]-4-oxobutanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]-3-carboxypropanoyl]amino]-3-hydroxybutanoyl]amino]-3-methylpentanoic acid	1253854: Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting	ki	0.0008	uM
3-[3-chloro-5-(trifluoromethyl)-2-pyridinyl]-N-(cyclopropylmethyl)-2,5-dimethyl-N-propylpyrazolo[1,5-a]pyrimidin-7-amine	238737: Binding affinity for recombinant human CRF1 receptor	ki	0.0008	uM

CTD chemical–gene interactions

29 total (human), top 29 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Acetaminophen	decreases expression, increases expression	2
Benzo(a)pyrene	decreases methylation, affects methylation	2
Tetrachlorodibenzodioxin	affects cotreatment, decreases expression, increases expression	2
propionaldehyde	decreases expression	1
potassium perchlorate	decreases expression	1
butyraldehyde	increases expression	1
ochratoxin A	increases expression, increases acetylation	1
pentanal	increases expression	1
tebuconazole	decreases expression	1
CGP 52608	affects binding, increases reaction	1
antalarmin	affects binding, decreases activity	1
astressin	affects binding, decreases activity	1
Grape Seed Proanthocyanidins	affects cotreatment, increases expression	1
2-methyl-2H-pyrazole-3-carboxylic acid (2-methyl-4-o-tolylazophenyl)amide	decreases expression, affects cotreatment	1
bisphenol S	decreases methylation	1
Resveratrol	decreases expression, affects cotreatment	1
Cyclic AMP	affects binding, increases abundance, increases activity, increases reaction	1
Catechin	affects cotreatment, increases expression	1
Diazinon	increases methylation	1
Estradiol	increases expression	1
Hydrogen Peroxide	decreases expression	1
Lead	increases expression	1
Plant Extracts	affects cotreatment, decreases expression	1
Progesterone	increases activity, increases reaction, increases abundance, increases expression, affects binding	1
Rifampin	decreases expression	1
Triazoles	affects binding, decreases activity	1
Valproic Acid	increases methylation	1
1-Methyl-4-phenylpyridinium	affects expression	1
Sodium Selenite	increases expression	1

ChEMBL screening assays

193 unique, capped per target: 139 binding, 54 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1004666	Binding	Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells	Synthesis and pharmacological characterization of novel druglike corticotropin-releasing factor 1 antagonists. — J Med Chem
CHEMBL1004667	Functional	Antagonist activity at human CRF1 receptor expressed in CHO cells assessed as effect on sauvagine-induced cAMP production	Synthesis and pharmacological characterization of novel druglike corticotropin-releasing factor 1 antagonists. — J Med Chem

Cellosaurus cell lines

6 cell lines: 4 spontaneously immortalized cell line, 1 transformed cell line, 1 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_C0SF	ACTOne CRHR1	Transformed cell line	Female
CVCL_H415	CHO-K1/CRF1/Galpha15	Spontaneously immortalized cell line	Female
CVCL_KU97	cAMP Hunter CHO-K1 CRHR1 Gs	Spontaneously immortalized cell line	Female
CVCL_KW74	PathHunter CHO-K1 CRHR1 beta-arrestin	Spontaneously immortalized cell line	Female
CVCL_LA08	PathHunter U2OS CRHR1 Activated GPCR Internalization	Cancer cell line	Female
CVCL_ZK50	GeneBLAzer CRHR1-CRE-bla CHO-K1	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT00376051	PHASE4	COMPLETED	Serotonergic Function and Behavioural and Psychological Symptoms of Frontotemporal Dementia
NCT00950430	PHASE4	ENROLLING_BY_INVITATION	Imaging of Brain Amyloid Plaques in the Aging Population
NCT06093126	PHASE4	RECRUITING	Lemborexant for Insomnia in a Patient With Dementia: An N-of-1 Trial
NCT00594737	PHASE3	COMPLETED	Open Label Pilot Study of the Effects of Memantine on FDG-PET in Frontotemporal Dementia
NCT03682185	PHASE3	COMPLETED	The Healthy Patterns Sleep Study
NCT04374136	PHASE3	TERMINATED	A Phase 3 Study to Evaluate Efficacy and Safety of AL001 in Frontotemporal Dementia (INFRONT-3)
NCT00416169	PHASE2	COMPLETED	A Pilot Study to Explore the Safety and Tolerability of Galantamine HBr in the Treatment of Pick Complex/Frontotemporal Dementia
NCT01890343	PHASE2	COMPLETED	Imaging Characteristics of Florbetapir 18F in Patients With Frontotemporal Dementia, Alzheimer’s Disease and Normal Controls.
NCT01937013	PHASE2	COMPLETED	Impact of Emotional Mimicry and Oxytocin on Frontotemporal Dementia
NCT02676843	PHASE2	COMPLETED	Tau PET Imaging With 18F-AV-1451 in Subjects With MAPT Mutations
NCT02862210	PHASE2	COMPLETED	Low-Dose Lithium for the Treatment of Behavioral Symptoms in Frontotemporal Dementia
NCT03260920	PHASE2	UNKNOWN	Intranasal Oxytocin for Frontotemporal Dementia
NCT03987295	PHASE2	COMPLETED	A Phase 2 Study to Evaluate Safety of Long-term AL001 Dosing in Frontotemporal Dementia (FTD) Patients (INFRONT-2)
NCT04220021	PHASE2	ACTIVE_NOT_RECRUITING	Safety and Therapeutic Potential of the FDA-approved Drug Metformin for C9orf72 ALS/FTD
NCT04489017	PHASE2	COMPLETED	Palmitoylethanolamide Combined With Luteoline in Frontotemporal Dementia Patients. A Randomized Controlled Trial
NCT04937452	PHASE2	COMPLETED	Dopaminergic Therapy for Frontotemporal Dementia Patients
NCT04993755	PHASE2	COMPLETED	A Phase 2a Study of TPN-101 in Patients With C9ORF72 ALS/FTD
NCT05742698	PHASE2	RECRUITING	Nabilone for Agitation in Frontotemporal Dementia
NCT06604520	PHASE2	RECRUITING	Vortioxetine for the Treatment of Mood and Cognitive Symptoms in Frontotemporal Dementia
NCT07154485	PHASE2	NOT_YET_RECRUITING	Investigator Initiated Study for the Safety and Efficacy in Frontotemporal Dementia
NCT01386333	PHASE1	COMPLETED	Safety Study of Intranasal Oxytocin in Frontotemporal Dementia
NCT03040713	PHASE1	COMPLETED	Flortaucipir PET Imaging in Subjects With FTD
NCT03636204	PHASE1	COMPLETED	A First in Human Study in Healthy Volunteers and in Participants With Frontotemporal Dementia With Granulin (GRN) Mutation
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NCT04747431	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	A Study of PBFT02 in Participants With FTD and Mutations in the Granulin Precursor (GRN) or C9ORF72 Genes
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NCT06064890	PHASE1/PHASE2	RECRUITING	A Study to Evaluate the Safety and Effect of AVB-101, a Gene Therapy Product, in Subjects With a Genetic Sub-type of Frontotemporal Dementia (FTD-GRN)
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NCT06891716	EARLY_PHASE1	RECRUITING	[18F]ACI-19626 PET in TDP-43 Proteinopathies
NCT00159198	Not specified	TERMINATED	Amyotrophic Lateral Sclerosis and Frontotemporal Dementia
NCT00938665	Not specified	COMPLETED	Evaluation of a Handheld Event Related Potential (ERP)/Quantitative Electroencephalography (qEEG) System (COGNISION™) as a Useful Cognitive Biomarker for Alzheimer’s Disease.
NCT01002300	Not specified	COMPLETED	Oxytocin and Social Cognition in Frontotemporal Dementia
NCT01147679	Not specified	UNKNOWN	Study of Social Behavior and Emotion in Frontotemporal Dementia, Alzheimer’s Disease and Controls