CRHR2
gene geneOn this page
Also known as CRF2CRF-RBHM-CRF
Summary
CRHR2 (corticotropin releasing hormone receptor 2, HGNC:2358) is a protein-coding gene on chromosome 7p14.3, encoding Corticotropin-releasing factor receptor 2 (Q13324). G-protein coupled receptor for CRH (corticotropin-releasing factor), UCN (urocortin), UCN2 and UCN3.
The protein encoded by this gene belongs to the G-protein coupled receptor 2 family, and the subfamily of corticotropin releasing hormone receptor. This receptor shows high affinity for corticotropin releasing hormone (CRH), and also binds CRH-related peptides such as urocortin. CRH is synthesized in the hypothalamus, and plays an important role in coordinating the endocrine, autonomic, and behavioral responses to stress and immune challenge. Studies in mice suggest that this receptor maybe involved in mediating cardiovascular homeostasis. Alternatively spliced transcript variants encoding different isoforms have been described for this gene.
Source: NCBI Gene 1395 — RefSeq curated summary.
At a glance
- GWAS associations: 2
- Clinical variants (ClinVar): 85 total
- Druggable target: yes
- MANE Select transcript:
NM_001883
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:2358 |
| Approved symbol | CRHR2 |
| Name | corticotropin releasing hormone receptor 2 |
| Location | 7p14.3 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | CRF2, CRF-RB, HM-CRF |
| Ensembl gene | ENSG00000106113 |
| Ensembl biotype | protein_coding |
| OMIM | 602034 |
| Entrez | 1395 |
Gene structure
Transcript identifiers
Ensembl transcripts: 9 — 6 protein_coding, 2 nonsense_mediated_decay, 1 protein_coding_CDS_not_defined
ENST00000341843, ENST00000348438, ENST00000423776, ENST00000445981, ENST00000452278, ENST00000462882, ENST00000471646, ENST00000506074, ENST00000942525
RefSeq mRNA: 5 — MANE Select: NM_001883
NM_001202475, NM_001202481, NM_001202482, NM_001202483, NM_001883
CCDS: CCDS5429, CCDS56477, CCDS56478, CCDS75576
Canonical transcript exons
ENST00000471646 — 12 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001839307 | 30651942 | 30653600 |
| ENSE00001850462 | 30682178 | 30682456 |
| ENSE00003525896 | 30681915 | 30682040 |
| ENSE00003534188 | 30655039 | 30655080 |
| ENSE00003569024 | 30665070 | 30665187 |
| ENSE00003618234 | 30660573 | 30660645 |
| ENSE00003619601 | 30662156 | 30662216 |
| ENSE00003626855 | 30667228 | 30667313 |
| ENSE00003642161 | 30655927 | 30656012 |
| ENSE00003651352 | 30662694 | 30662847 |
| ENSE00003653965 | 30665530 | 30665639 |
| ENSE00003666810 | 30655580 | 30655715 |
Expression profiles
Bgee: expression breadth ubiquitous, 158 present calls, max score 86.85.
FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.3363 / max 38.0836, expressed in 152 samples.
FANTOM5 promoters (2 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 83456 | 0.1874 | 88 |
| 83455 | 0.1489 | 92 |
Top tissues by expression
283 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 86.85 | silver quality |
| endometrium epithelium | UBERON:0004811 | 84.64 | gold quality |
| ganglionic eminence | UBERON:0004023 | 82.94 | gold quality |
| ventricular zone | UBERON:0003053 | 82.83 | gold quality |
| paraflocculus | UBERON:0005351 | 81.53 | gold quality |
| frontal pole | UBERON:0002795 | 81.50 | gold quality |
| middle frontal gyrus | UBERON:0002702 | 80.51 | gold quality |
| tibialis anterior | UBERON:0001385 | 73.38 | silver quality |
| apex of heart | UBERON:0002098 | 73.07 | gold quality |
| adenohypophysis | UBERON:0002196 | 71.63 | gold quality |
| pituitary gland | UBERON:0000007 | 70.29 | gold quality |
| embryo | UBERON:0000922 | 69.64 | gold quality |
| hindlimb stylopod muscle | UBERON:0004252 | 66.78 | gold quality |
| right frontal lobe | UBERON:0002810 | 66.73 | gold quality |
| heart left ventricle | UBERON:0002084 | 66.13 | gold quality |
| cortical plate | UBERON:0005343 | 65.51 | gold quality |
| cardiac ventricle | UBERON:0002082 | 65.27 | gold quality |
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 65.16 | gold quality |
| prefrontal cortex | UBERON:0000451 | 64.75 | gold quality |
| Brodmann (1909) area 9 | UBERON:0013540 | 64.36 | gold quality |
| colonic epithelium | UBERON:0000397 | 64.23 | silver quality |
| cingulate cortex | UBERON:0003027 | 63.68 | gold quality |
| cerebellar vermis | UBERON:0004720 | 63.67 | gold quality |
| anterior cingulate cortex | UBERON:0009835 | 63.54 | gold quality |
| lower esophagus mucosa | UBERON:0035834 | 63.26 | gold quality |
| dorsolateral prefrontal cortex | UBERON:0009834 | 62.96 | gold quality |
| body of pancreas | UBERON:0001150 | 62.85 | gold quality |
| neocortex | UBERON:0001950 | 62.83 | gold quality |
| right coronary artery | UBERON:0001625 | 62.57 | gold quality |
| frontal cortex | UBERON:0001870 | 62.53 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 0.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | no | 3.07 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): UCN
miRNA regulators (miRDB)
33 targeting CRHR2, 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-6867-5P | 100.00 | 82.21 | 3464 |
| HSA-MIR-5582-3P | 99.86 | 72.48 | 4221 |
| HSA-MIR-1323 | 99.83 | 69.89 | 2471 |
| HSA-MIR-548O-3P | 99.74 | 69.30 | 2228 |
| HSA-MIR-29B-2-5P | 99.67 | 68.98 | 1726 |
| HSA-MIR-4328 | 99.57 | 71.06 | 4094 |
| HSA-MIR-671-5P | 99.52 | 67.11 | 1277 |
| HSA-MIR-4505 | 99.27 | 67.81 | 2678 |
| HSA-MIR-149-5P | 99.25 | 67.16 | 1315 |
| HSA-MIR-5787 | 99.22 | 67.86 | 2628 |
| HSA-MIR-6791-5P | 99.16 | 65.92 | 1844 |
| HSA-MIR-4705 | 99.10 | 69.10 | 1091 |
| HSA-MIR-661 | 99.09 | 65.94 | 2062 |
| HSA-MIR-1228-3P | 99.00 | 66.53 | 857 |
| HSA-MIR-4774-3P | 98.90 | 67.82 | 737 |
| HSA-MIR-873-5P | 98.84 | 66.90 | 1348 |
| HSA-MIR-423-5P | 98.69 | 67.48 | 1522 |
| HSA-MIR-3184-5P | 98.56 | 67.13 | 1491 |
| HSA-MIR-7114-5P | 98.51 | 67.87 | 1349 |
| HSA-MIR-3166 | 98.24 | 66.63 | 1223 |
| HSA-MIR-3179 | 98.22 | 65.90 | 1445 |
| HSA-MIR-596 | 97.48 | 63.13 | 469 |
| HSA-MIR-3121-5P | 97.30 | 66.62 | 1146 |
| HSA-MIR-4726-5P | 97.24 | 65.67 | 1299 |
| HSA-MIR-3116 | 97.07 | 65.78 | 1324 |
| HSA-MIR-6894-3P | 96.73 | 65.64 | 798 |
| HSA-MIR-563 | 96.26 | 66.13 | 450 |
| HSA-MIR-380-5P | 95.68 | 67.32 | 512 |
| HSA-MIR-6823-3P | 95.45 | 66.14 | 704 |
| HSA-MIR-4268 | 94.45 | 64.09 | 819 |
Literature-anchored findings (GeneRIF, showing 40)
- 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)
- data suggest a distinctive role for corticotropin-releasing hormone receptor 2 specific agonists like urocortin II in the control of myometrial contractility during human pregnancy (PMID:14592950)
- 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)
- The regions of the CRF2(a) promoter that regulate the inducible expression were determined (PMID:15331578)
- ligand binding properties of CRFR2 (PMID:15652653)
- There is no significant difference between the expression of CRH-R2beta mRNA of preeclampsia and of normal pregnancies. (PMID:15924674)
- expression by semiquantitative reverse transcriptase-polymerase chain reaction (RT-PCR) and fluorescent immunocytochemistry in umbilical cord blood-derived cultured mast cells (PMID:16326828)
- CRHR2 polymorphisms examined do not confer susceptibility to panic disorder. (PMID:16691126)
- 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; the most pronounced down-regulation of CRH-BP and CRH-R2 occurred in laboring cervix, irrespective the length of gestation (PMID:16734917)
- Results demonstrate corticotropin-releasing factor (2) expression in the human gastric mucosa and indicate a physiological role of this receptor type in regulating apoptosis, an important parameter of gastric cell regeneration. (PMID:16972272)
- Both CRHR1 and CRHR2 play a facilitatory role in the non-clathrin-, non-caveolae-mediated endocytosis and intracellular signal transduction of urocortin. (PMID:17170072)
- 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)
- results show that haplotype variation at the CRHR2 locus is associated with suicidal behaviour (PMID:17532191)
- Human myometrium expresses both CRH-R1 and CRH-R2 during pregnancy. (PMID:17959885)
- Cultured placental trophoblasts express both CRH-R1 and CRH-R2. (PMID:18325997)
- Association of corticotropin-releasing hormone receptor-2 genetic variants with acute bronchodilator response in asthma. (PMID:18408560)
- UCN inhibited the proliferation and promoted the apoptosis of endothelial cells and down-regulated VEGF expression in vivo via CRFR2. (PMID:18443956)
- Expression loss of CRFR2 in prostate cancer and its neovascularization contributes to prostate tumorigenesis, progression, and neoangiogenesis. (PMID:19058138)
- receptors couple to different G-proteins in stably transfected human cells, leading to transient divalent calcium ion mobilization on top of the natural increase in cyclic AMP stimulation. (PMID:19098121)
- the SCP/CRHR2 system is present in human ovaries and treatment with SCP/Ucn3 inhibits progesterone production by cultured granulosa-lutein cells through interaction with CRHR2 (PMID:19351656)
- Trophoblast cell cultures treated with increasing amounts of type 2 corticotrophin releasing hormone receptor mediate increased secretion of estradiol in the presence of androstenedione. (PMID:19417223)
- CRH-R1 and CRH-R2 receptors and their endogenous ligands have a role in the biology of human endometrial cancer. (PMID:19433256)
- nuclear translocation of Ucn along with the loss of CRFR2 in epithelial cells and microvasculature of tumoral specimens may be involved in the pathobiology of renal cell carcinoma (PMID:19437022)
- Results suggest that the rs2267716 polymorphism in the CRHR2 gene might influence the risk of developing HCC in patients with HBV infection in Chinese population. (PMID:19813023)
- Investigated whether a genetic variation in CRHR2 gene might be associated with preterm birth. The polymorphism does not increase the risk for preterm birth overall but might modulate the length of pregnancy in a dose dependent fashion in Caucasian women. (PMID:20164545)
- cross-talk between corticotropin-releasing factor (CRF) and muscarinic receptors (PMID:20594969)
- both CRF receptors were found in breast cancer and the respective benign adjacent tissue. The two CRF receptor proteins presented distinct distribution and subcellular localization, pointing into differing biological roles. (PMID:20630588)
- Structural basis for hormone recognition by the Human CRFR2{alpha} G protein-coupled receptor. (PMID:20966082)
- These findings reveal a complex interplay between the signaling molecules that allow “fine-tuning” of CRH-R2beta functional responses and regulate signal integration. (PMID:21338628)
- data suggest a prominent role of CRF(1) in stressor-induced changes in EtOH consumption, with involvement of CRF(2) in recovery from stressor effects (PMID:21487655)
- in placenta, CRH produced locally regulates GLUT1 and GLUT3 expression, CRHR1 and CRHR2-mediated differential regulation of GLUT1 and GLUT3 expression (PMID:22234467)
- 12 single nucleotide polymorphisms (SNPs) CRHR1 and CRHR2 in major depressive disorder patients (n = 173), panic disorder patients (n = 180), and healthy controls, were investigated. (PMID:22467522)
- Suggest that urocortin 1 increase LPS-induced endothelial permeability by disrupting the VE-cadherin-beta-catenin complex via activation of CRHR2. (PMID:23168683)
- Polymorphisms within CRHR1 and CRHR2 genes interacted with both childhood sexual abuse and emotional neglect to influence Iowa Gambling Task performance. (PMID:23177644)
- The down-regulation of the CRF2 receptor in the distal/sigmoid biopsies of ulcerative colitis patients is indicative of change in CRF2 signalling associated with the process of inflammation. (PMID:23539366)
- The rate and extent of homologous CRF2(a) receptor desensitization is governed by agonist-specific mechanisms affecting G protein-coupled receptor kinase phosphorylation. (PMID:23820308)
- Data indicate that estrogen increased the abundance of the mRNA encoding CRH-R2 and an alternative splice variant encoding CRH-R1 in which exon 12 was deleted [CRH-R1(Delta12)]. (PMID:23821771)
- These results fail to provide support for an association of CRHR1 and CRHR2 with personality traits in a Japanese adult population. (PMID:23982282)
- CRFR2 antagonist astressin-2B abrogated the effects of UCN2 on VSMCs. In conclusion, UCN2 is significantly associated with AAA and inhibits VSMC proliferation by inducing a G1 cell cycle arrest suggesting a plausible regulatory role in AAA pathogenesis (PMID:24107226)
Cross-species orthologs
3 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | CRHR2 | ENSDARG00000062377 |
| mus_musculus | Crhr2 | ENSMUSG00000003476 |
| rattus_norvegicus | Crhr2 | ENSRNOG00000011145 |
Paralogs (42): CALCR (ENSG00000004948), GIPR (ENSG00000010310), ADGRA2 (ENSG00000020181), CALCRL (ENSG00000064989), GLP2R (ENSG00000065325), ADGRF5 (ENSG00000069122), ADGRL1 (ENSG00000072071), ADCYAP1R1 (ENSG00000078549), SCTR (ENSG00000080293), VIPR2 (ENSG00000106018), GHRHR (ENSG00000106128), ADGRD1 (ENSG00000111452), GLP1R (ENSG00000112164), ADGRG6 (ENSG00000112414), VIPR1 (ENSG00000114812), ADGRL2 (ENSG00000117114), CRHR1 (ENSG00000120088), ADGRB2 (ENSG00000121753), ADGRE5 (ENSG00000123146), ADGRE2 (ENSG00000127507), ADGRE3 (ENSG00000131355), ADGRB3 (ENSG00000135298), PTH2R (ENSG00000144407), ADGRG7 (ENSG00000144820), ADGRL3 (ENSG00000150471), ADGRA3 (ENSG00000152990), ADGRF1 (ENSG00000153292), ADGRF4 (ENSG00000153294), ADGRG4 (ENSG00000156920), ADGRG5 (ENSG00000159618), 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 2 — Q13324 (reviewed: Q13324)
Alternative names: Corticotropin-releasing hormone receptor 2
All UniProt accessions (4): Q13324, A0A090N7T4, C9JZM9, F2Z2M6
UniProt curated annotations — full annotation on UniProt →
Function. G-protein coupled receptor for CRH (corticotropin-releasing factor), UCN (urocortin), UCN2 and UCN3. Has high affinity for 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.
Subunit / interactions. Monomer. Interacts (via N-terminal extracellular domain) with CRF, UCN, UCN2 and UCN3. Has highest affinity for UCN, and considerably lower affinity for CRF, UNC2 and UCN3.
Subcellular location. Cell membrane.
Post-translational modifications. A N-glycosylation site within the signal peptide impedes its proper cleavage and function.
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 uncleaved pseudo signal peptide prevents receptor’s oligomerization and coupling to G(i) subunits. It is also responsible for the rather low receptor localization at the plasma membrane.
Similarity. Belongs to the G-protein coupled receptor 2 family.
Isoforms (7)
| UniProt ID | Names | Canonical? |
|---|---|---|
| Q13324-1 | CRF2-alpha | yes |
| Q13324-2 | CRF2-beta | |
| Q13324-3 | CRF2-gamma | |
| Q13324-4 | D | |
| Q13324-5 | E | |
| Q13324-6 | F | |
| Q13324-7 | desQ |
RefSeq proteins (5): NP_001189404, NP_001189410, NP_001189411, NP_001189412, NP_001874* (*=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 |
| IPR003053 | GPCR_2_CRF2_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 (59 total): helix 16, topological domain 8, transmembrane region 7, splice variant 6, glycosylation site 5, disulfide bond 5, strand 5, sequence conflict 2, turn 2, chain 1, signal peptide 1, sequence variant 1
Structure
Experimental structures (PDB)
6 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 3N93 | X-RAY DIFFRACTION | 2.5 |
| 3N95 | X-RAY DIFFRACTION | 2.72 |
| 3N96 | X-RAY DIFFRACTION | 2.75 |
| 6PB1 | ELECTRON MICROSCOPY | 2.8 |
| 7TS0 | ELECTRON MICROSCOPY | 2.8 |
| 7TRY | ELECTRON MICROSCOPY | 3.7 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q13324-F1 | 78.80 | 0.21 |
Antibody-complex structures (SAbDab): 3 — 6PB1, 7TRY, 7TS0
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Disulfide bonds (5): 14–50, 40–83, 64–98, 184–254, 51–77
Glycosylation sites (5): 13, 41, 74, 86, 94
Function
Pathways and Gene Ontology
Reactome pathways
3 pathways
| ID | Pathway |
|---|---|
| R-HSA-418555 | G alpha (s) signalling events |
| R-HSA-422085 | Synthesis, secretion, and deacylation of Ghrelin |
| R-HSA-373080 | Class B/2 (Secretin family receptors) |
MSigDB gene sets: 119 (showing top):
MORF_RAGE, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, XU_GH1_AUTOCRINE_TARGETS_UP, MODULE_45, MODULE_64, GRAESSMANN_APOPTOSIS_BY_SERUM_DEPRIVATION_DN, MODULE_16, GOBP_CELLULAR_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, GOBP_CELL_CELL_SIGNALING, BROWNE_HCMV_INFECTION_48HR_DN, GOBP_ADENYLATE_CYCLASE_MODULATING_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, GOBP_HORMONE_MEDIATED_SIGNALING_PATHWAY, GOBP_REGULATION_OF_SYNAPTIC_PLASTICITY, GOBP_CELLULAR_RESPONSE_TO_HORMONE_STIMULUS, MORF_FANCG
GO Biological Process (7): cell surface receptor signaling pathway (GO:0007166), adenylate cyclase-modulating G protein-coupled receptor signaling pathway (GO:0007188), long-term synaptic potentiation (GO:0060291), signal transduction (GO:0007165), G protein-coupled receptor signaling pathway (GO:0007186), hormone-mediated signaling pathway (GO:0009755), cellular response to corticotropin-releasing hormone stimulus (GO:0071376)
GO Molecular Function (7): G protein-coupled peptide receptor activity (GO:0008528), corticotrophin-releasing factor receptor activity (GO:0015056), peptide hormone binding (GO:0017046), corticotropin-releasing hormone receptor activity (GO:0043404), transmembrane signaling receptor activity (GO:0004888), G protein-coupled receptor activity (GO:0004930), protein binding (GO:0005515)
GO Cellular Component (4): plasma membrane (GO:0005886), dendrite (GO:0030425), axon terminus (GO:0043679), membrane (GO:0016020)
Reactome top-level categories
Rollup of top-3 pathways:
| Category | Pathways |
|---|---|
| GPCR downstream signalling | 1 |
| Peptide hormone metabolism | 1 |
| GPCR ligand binding | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| signal transduction | 3 |
| G protein-coupled receptor activity | 3 |
| G protein-coupled receptor signaling pathway | 2 |
| signaling receptor activity | 2 |
| adenylate cyclase activity | 1 |
| regulation of synaptic plasticity | 1 |
| positive regulation of synaptic transmission | 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 corticotropin-releasing hormone | 1 |
| cellular response to peptide hormone stimulus | 1 |
| peptide receptor activity | 1 |
| cellular response to corticotropin-releasing hormone stimulus | 1 |
| hormone binding | 1 |
| hormone-mediated signaling pathway | 1 |
| corticotropin-releasing hormone binding | 1 |
| transmembrane signaling receptor activity | 1 |
| binding | 1 |
| membrane | 1 |
| cell periphery | 1 |
| neuron projection | 1 |
| dendritic tree | 1 |
| neuron projection terminus | 1 |
| presynapse | 1 |
| distal axon | 1 |
| cellular anatomical structure | 1 |
Protein interactions and networks
STRING
1098 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| CRHR2 | UCN2 | Q96RP3 | 999 |
| CRHR2 | CRH | P06850 | 999 |
| CRHR2 | UCN | P55089 | 999 |
| CRHR2 | UCN3 | Q969E3 | 999 |
| CRHR2 | CRHBP | P24387 | 973 |
| CRHR2 | POMC | P01189 | 895 |
| CRHR2 | MC2R | Q01718 | 688 |
| CRHR2 | PDYN | P01213 | 676 |
| CRHR2 | IGFBP2 | P18065 | 646 |
| CRHR2 | NR3C1 | P04150 | 615 |
| CRHR2 | SCT | P09683 | 599 |
| CRHR2 | VIP | P01282 | 587 |
| CRHR2 | ADCYAP1 | P18509 | 577 |
| CRHR2 | OXT | P01178 | 567 |
| CRHR2 | NR3C2 | P08235 | 566 |
IntAct
7 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| CRHR2 | RAMP1 | psi-mi:“MI:0915”(physical association) | 0.400 |
| CRHR2 | RAMP3 | psi-mi:“MI:0915”(physical association) | 0.400 |
| RAMP3 | CRHR2 | psi-mi:“MI:0915”(physical association) | 0.400 |
| CRHR2 | RAMP2 | psi-mi:“MI:0915”(physical association) | 0.400 |
| CRHR2 | GPR35 | psi-mi:“MI:0915”(physical association) | 0.370 |
BioGRID (5): MALL (Two-hybrid), CRHR2 (Reconstituted Complex), CRHR2 (Two-hybrid), Ucn (Reconstituted Complex), APP (Reconstituted Complex)
ESM2 similar proteins: B0BM39, B3VSC2, B5X3I6, F7BWT7, O14494, O14817, O35566, O42602, O42603, O43688, O60636, O62772, O75954, O88956, O95857, O95858, P35353, P47866, P48509, P60588, Q01453, Q06AA5, Q13324, Q3SYV5, Q3ZBV0, Q4L208, Q5RAP3, Q5RAZ3, Q5ZJ75, Q60748, Q6DCQ3, Q6GMK6, Q6WL85, Q86UF1, Q8BJU2, Q8K593, Q8R3S2, Q8R4D1, Q90812, Q91ZH7
Diamond homologs: A0A2Z2U4G9, A6QP74, O35659, O42602, O42603, O46502, O62772, O95838, P23811, P25107, P25117, P25961, P30082, P30083, P32082, P32215, P32241, P32301, P34998, P34999, P35000, P35347, P35353, P41586, P41587, P41588, P41593, P43218, P43219, P43220, P47866, P47871, P47872, P48546, P48960, P49190, P50133, P70205, P70555, P97751
SIGNOR signaling
12 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| “GABA-A (a1-b1-g2) receptor” | down-regulates | CRHR2 | |
| “GABA-A (a2-b1-g2) receptor” | down-regulates | CRHR2 | |
| “GABA-A (a3-b1-g2) receptor” | down-regulates | CRHR2 | |
| “GABA-A (a4-b1-g2) receptor” | down-regulates | CRHR2 | |
| “GABA-A (a4-b2-d) receptor” | down-regulates | CRHR2 | |
| “GABA-A (a4-b3-d) receptor” | down-regulates | CRHR2 | |
| “GABA-A (a5-b1-g2) receptor” | down-regulates | CRHR2 | |
| “GABA-A (a6-b1-g2) receptor” | down-regulates | CRHR2 | |
| “GABA-A (a6-b2-d) receptor” | down-regulates | CRHR2 | |
| “GABA-A (a6-b3-d) receptor” | down-regulates | CRHR2 | |
| GABA-A | down-regulates | CRHR2 | |
| CRH | “up-regulates activity” | CRHR2 | binding |
Disease & clinical
Clinical variants and AI predictions
ClinVar
85 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 71 |
| Likely benign | 6 |
| Benign | 2 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
2472 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 7:30655077:AACCC:A | acceptor_loss | 1.0000 |
| 7:30655078:ACCC:A | acceptor_loss | 1.0000 |
| 7:30655079:CCCTG:C | acceptor_loss | 1.0000 |
| 7:30655080:CCT:C | acceptor_loss | 1.0000 |
| 7:30655081:C:CA | acceptor_loss | 1.0000 |
| 7:30655082:T:A | acceptor_loss | 1.0000 |
| 7:30655923:ATAC:A | donor_loss | 1.0000 |
| 7:30655924:TA:T | donor_loss | 1.0000 |
| 7:30655925:ACCTG:A | donor_loss | 1.0000 |
| 7:30655926:C:A | donor_loss | 1.0000 |
| 7:30656008:TTGAT:T | acceptor_gain | 1.0000 |
| 7:30656025:C:CT | acceptor_gain | 1.0000 |
| 7:30656026:G:T | acceptor_gain | 1.0000 |
| 7:30656029:C:CT | acceptor_gain | 1.0000 |
| 7:30656030:A:AC | acceptor_gain | 1.0000 |
| 7:30656030:A:C | acceptor_gain | 1.0000 |
| 7:30660567:GCTTA:G | donor_loss | 1.0000 |
| 7:30660568:CTTAC:C | donor_loss | 1.0000 |
| 7:30660569:TTAC:T | donor_loss | 1.0000 |
| 7:30660570:TA:T | donor_loss | 1.0000 |
| 7:30660571:A:T | donor_loss | 1.0000 |
| 7:30662149:CACTT:C | donor_loss | 1.0000 |
| 7:30662150:ACTT:A | donor_loss | 1.0000 |
| 7:30662152:TTA:T | donor_loss | 1.0000 |
| 7:30662153:TAC:T | donor_loss | 1.0000 |
| 7:30662154:A:AC | donor_gain | 1.0000 |
| 7:30662154:ACTGT:A | donor_loss | 1.0000 |
| 7:30662155:C:CG | donor_gain | 1.0000 |
| 7:30662155:CT:C | donor_gain | 1.0000 |
| 7:30662155:CTG:C | donor_gain | 1.0000 |
AlphaMissense
2695 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 7:30667276:C:A | W89C | 1.000 |
| 7:30667276:C:G | W89C | 1.000 |
| 7:30681991:C:A | W51C | 1.000 |
| 7:30681991:C:G | W51C | 1.000 |
| 7:30665149:A:G | L155P | 0.999 |
| 7:30667250:C:G | C98S | 0.999 |
| 7:30667251:A:T | C98S | 0.999 |
| 7:30667278:A:G | W89R | 0.999 |
| 7:30667278:A:T | W89R | 0.999 |
| 7:30667295:C:G | C83S | 0.999 |
| 7:30667296:A:T | C83S | 0.999 |
| 7:30667301:C:G | R81P | 0.999 |
| 7:30681993:A:G | W51R | 0.999 |
| 7:30681993:A:T | W51R | 0.999 |
| 7:30655080:C:G | G352R | 0.998 |
| 7:30655675:C:G | G320R | 0.998 |
| 7:30655689:A:T | L315H | 0.998 |
| 7:30662190:A:G | W242R | 0.998 |
| 7:30662190:A:T | W242R | 0.998 |
| 7:30662697:A:G | W232R | 0.998 |
| 7:30662697:A:T | W232R | 0.998 |
| 7:30662790:A:G | W201R | 0.998 |
| 7:30662790:A:T | W201R | 0.998 |
| 7:30667251:A:G | C98R | 0.998 |
| 7:30667296:A:G | C83R | 0.998 |
| 7:30681953:C:G | C64S | 0.998 |
| 7:30681954:A:G | C64R | 0.998 |
| 7:30681954:A:T | C64S | 0.998 |
| 7:30655683:G:C | P317R | 0.997 |
| 7:30656007:A:C | N279K | 0.997 |
dbSNP variants (sampled 300 via entrez): RS1000001973 (7:30653181 A>C), RS1000046878 (7:30664045 C>T), RS1000096222 (7:30678733 C>T), RS1000133113 (7:30694677 A>C), RS1000313121 (7:30669272 T>C), RS1000342158 (7:30682856 A>T), RS1000442020 (7:30676849 G>A,T), RS1000482166 (7:30699381 C>T), RS1000488730 (7:30699664 A>G), RS1000516084 (7:30670566 A>G), RS1000552916 (7:30677980 G>A), RS1000567769 (7:30659241 G>T), RS1000576664 (7:30653687 G>C,T), RS1000653204 (7:30670898 C>A,T), RS1000683013 (7:30684549 C>G)
Disease associations
OMIM: gene MIM:602034 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
2 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST002352_30 | Type 2 diabetes | 8.000000e-06 |
| GCST009379_68 | Type 2 diabetes | 4.000000e-11 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (2): CHEMBL3885546 (PROTEIN COMPLEX), CHEMBL4069 (SINGLE PROTEIN)
PharmGKB: 1 entry (VIP=true, CPIC=false)
PharmGKB clinical annotations
5 annotations.
| Variant | Type | Level | Drugs | Phenotypes |
|---|---|---|---|---|
| rs2267715 | Efficacy | 3 | salbutamol;selective beta-2-adrenoreceptor agonists | Asthma |
| rs2270007 | Efficacy | 3 | citalopram | Major Depressive Disorder |
| rs2284220 | Efficacy | 4 | salbutamol;selective beta-2-adrenoreceptor agonists | Asthma |
| rs255100 | Efficacy | 4 | salbutamol;selective beta-2-adrenoreceptor agonists | Asthma |
| rs7793837 | Efficacy | 3 | salbutamol | Asthma |
PharmGKB variants
6 variants.
| Variant | Genes | Level | Score | #Clin annots | Drugs |
|---|---|---|---|---|---|
| rs255100 | CRHR2 | 4 | -0.75 | 1 | salbutamol;selective beta-2-adrenoreceptor agonists |
| rs2267715 | CRHR2 | 3 | 0.75 | 1 | salbutamol;selective beta-2-adrenoreceptor agonists |
| rs2270007 | CRHR2 | 3 | 3.00 | 1 | citalopram |
| rs2284220 | CRHR2 | 4 | -1.25 | 1 | salbutamol;selective beta-2-adrenoreceptor agonists |
| rs7793837 | CRHR2 | 3 | 2.75 | 1 | salbutamol |
| rs73294475 | CRHR2 | 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 (20 total), top 20:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| [125I]urocortin 1 (mouse, rat) | Full agonist | 10.0 | pKd |
| [125I]antisauvagine | Antagonist | 9.9 | pKd |
| [125I]sauvagine (frog) | Full agonist | 9.8 | pKd |
| [125I]astressin | Antagonist | 9.7 | pKi |
| urocortin 1 | Full agonist | 9.6 | pKd |
| antisauvagine | Antagonist | 9.6 | pKd |
| urocortin 1 | Full agonist | 9.4 | pKd |
| sauvagine | Full agonist | 9.3 | pKd |
| urocortin 2 | Full agonist | 9.2 | pKd |
| K41498 | Antagonist | 9.2 | pKi |
| α-helical CRF | Antagonist | 9.1 | pKd |
| urotensin 1 (fish) | Full agonist | 8.9 | pKd |
| astressin | Antagonist | 8.9 | pKd |
| astressin 2B | Antagonist | 8.89 | pIC50 |
| K31440 | Antagonist | 8.8 | pKi |
| urocortin 3 | Full agonist | 8.7 | pKd |
| urocortin 2 | Full agonist | 8.6 | pKd |
| urocortin 3 | Full agonist | 8.0 | pKd |
| corticotrophin-releasing hormone | Full agonist | 7.4 | pKd |
| corticotropin-releasing factor | Full agonist | 6.9 | pKd |
Binding affinities (BindingDB)
7 measured of 7 human assays (7 total across all organisms); most potent 7 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| 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-[[[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 |
| 2-chloro-N-[4-[[4-chloro-3-(hydroxymethyl)pyrazol-1-yl]methyl]cyclohexyl]-5-(trifluoromethyl)benzamide | IC50 | 95 nM | US-8835444: Cyclohexyl amide derivatives as CRF receptor antagonists |
| 5-chloro-2-methyl-N-[4-[(5-methyl-3-phenylpyrazol-1-yl)methyl]cyclohexyl]pyridine-3-carboxamide | IC50 | 131 nM | US-8835444: Cyclohexyl amide derivatives as CRF receptor antagonists |
| 5-chloro-N-[4-[[(5-ethyl-4-methyl-1H-pyrazol-3-yl)amino]methyl]cyclohexyl]-2-methylpyridine-3-carboxamide | IC50 | 134 nM | US-8835444: Cyclohexyl amide derivatives as CRF receptor antagonists |
| 5-chloro-2-methyl-N-[4-[(5-methyl-3-pyridin-3-ylpyrazol-1-yl)methyl]cyclohexyl]pyridine-3-carboxamide | IC50 | 142 nM | US-8835444: Cyclohexyl amide derivatives as CRF receptor antagonists |
| 5-chloro-N-[4-[[3-(4-fluorophenyl)-5-methylpyrazol-1-yl]methyl]cyclohexyl]-2-methylpyridine-3-carboxamide | IC50 | 180 nM | US-8835444: Cyclohexyl amide derivatives as CRF receptor antagonists |
ChEMBL bioactivities
578 potent at pChembl≥5 of 868 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 9.49 | EC50 | 0.32 | nM | CHEMBL427807 |
| 9.38 | IC50 | 0.42 | nM | CHEMBL2368116 |
| 9.29 | IC50 | 0.51 | nM | CHEMBL2370929 |
| 9.24 | IC50 | 0.57 | nM | CHEMBL2370916 |
| 9.22 | IC50 | 0.6 | nM | CHEMBL2370926 |
| 9.21 | IC50 | 0.62 | nM | CHEMBL1794009 |
| 9.21 | IC50 | 0.61 | nM | CHEMBL2370933 |
| 9.14 | IC50 | 0.72 | nM | CHEMBL2370938 |
| 9.04 | IC50 | 0.92 | nM | CHEMBL2370927 |
| 8.96 | IC50 | 1.1 | nM | CHEMBL2370915 |
| 8.92 | IC50 | 1.2 | nM | CHEMBL2370939 |
| 8.90 | Ki | 1.26 | nM | CHEMBL2373995 |
| 8.89 | IC50 | 1.3 | nM | CHEMBL2370917 |
| 8.89 | IC50 | 1.3 | nM | CHEMBL2370940 |
| 8.85 | EC50 | 1.4 | nM | CHEMBL429560 |
| 8.82 | EC50 | 1.5 | nM | CHEMBL2373995 |
| 8.80 | IC50 | 1.6 | nM | SAUVAGINE |
| 8.72 | IC50 | 1.9 | nM | CHEMBL2370914 |
| 8.56 | Ki | 2.73 | nM | CHEMBL429560 |
| 8.44 | Ki | 3.6 | nM | CHEMBL427807 |
| 8.31 | IC50 | 4.9 | nM | CHEMBL2369694 |
| 8.30 | IC50 | 5 | nM | CHEMBL2369741 |
| 8.26 | IC50 | 5.5 | nM | CHEMBL2370931 |
| 8.21 | IC50 | 6.2 | nM | CHEMBL2370930 |
| 8.21 | IC50 | 6.2 | nM | HUMAN CORTICOTROPIN RELEASING FACTOR |
| 8.00 | IC50 | 10 | nM | CHEMBL1794010 |
| 7.91 | Ki | 12.2 | nM | CHEMBL2372650 |
| 7.88 | EC50 | 13.2 | nM | CHEMBL2372650 |
| 7.75 | IC50 | 17.8 | nM | CHEMBL2370920 |
| 7.38 | EC50 | 42 | nM | CHEMBL128100 |
| 7.34 | IC50 | 46 | nM | CHEMBL1794007 |
| 7.22 | IC50 | 60 | nM | CHEMBL2369693 |
| 7.21 | EC50 | 61.9 | nM | CHEMBL1077301 |
| 7.16 | IC50 | 69 | nM | LENEAR ASTRESSIN |
| 7.09 | IC50 | 81 | nM | CHEMBL2370924 |
| 7.06 | Ki | 86.4 | nM | CHEMBL1077301 |
| 6.59 | IC50 | 256 | nM | CHEMBL3731280 |
| 6.53 | IC50 | 296 | nM | CHEMBL3733118 |
| 6.34 | EC50 | 460 | nM | CHEMBL1995565 |
| 6.30 | IC50 | 506 | nM | CHEMBL1400385 |
| 6.26 | IC50 | 545 | nM | CHEMBL1375451 |
| 6.26 | EC50 | 544 | nM | CHEMBL1500274 |
| 6.21 | IC50 | 610 | nM | CHEMBL1489517 |
| 6.15 | EC50 | 709 | nM | CHEMBL1464584 |
| 6.14 | IC50 | 727 | nM | CHEMBL1974381 |
| 6.14 | IC50 | 723 | nM | CHEMBL1371902 |
| 6.14 | IC50 | 727 | nM | CHEMBL3681374 |
| 6.12 | IC50 | 754 | nM | CHEMBL1734544 |
| 6.10 | EC50 | 793 | nM | CHEMBL1526609 |
| 6.09 | IC50 | 811 | nM | CHEMBL3729075 |
PubChem BioAssay actives
37 with measured affinity, of 378 total; 31 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 |
|---|---|---|---|---|
| (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 | 223371: Activity of peptidic agonists on h-CRF2-alpha receptor using agonist-stimulated adenylate cyclase assay | ec50 | 0.0003 | uM |
| (4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(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-[[(2R)-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]-4-carboxybutanoyl]amino]-6-aminohexanoyl]amino]-4-carboxybutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R,3R)-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]amino]-1,4-dioxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoic acid | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0004 | uM |
| (4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-acetamido-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]-1-oxohexan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-amino-1,4-dioxobutan-2-yl]amino]-5-amino-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(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-[[(2R)-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]-4-carboxybutanoyl]amino]-6-aminohexanoyl]amino]-4-carboxybutanoyl]amino]-5-oxopentanoic acid | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0005 | 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 | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0006 | uM |
| (4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(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-[[(2R)-2-[[(2S)-2-[[(2R)-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]-4-carboxybutanoyl]amino]-6-aminohexanoyl]amino]-4-carboxybutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(3R,6S,9S,18R)-18-[[(2S)-1-[[(2S)-1-[[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]carbamoyl]-6-(2-amino-2-oxoethyl)-3-[3-(diaminomethylideneamino)propyl]-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoic acid | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0006 | uM |
| (4S)-4-amino-5-[[2-[(2S)-2-[(2S)-2-[[(2S,3S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(3R,6S,9S,18S)-18-[[(2S)-4-amino-1-[[(2S)-4-amino-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-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]amino]-1,4-dioxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]-methylcarbamoyl]-6-(3-amino-3-oxopropyl)-3-methyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-5-oxopentanoic acid | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0006 | uM |
| (4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-acetamido-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]-1-oxohexan-2-yl]amino]-4-amino-1,4-dioxobutan-2-yl]amino]-4-amino-1,4-dioxobutan-2-yl]amino]-5-amino-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(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-[[(2R)-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]-4-carboxybutanoyl]amino]-6-aminohexanoyl]amino]-4-carboxybutanoyl]amino]-5-oxopentanoic acid | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0006 | uM |
| (4S)-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-acetamido-1-[[(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]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-amino-1,5-dioxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-6-amino-1-oxohexan-2-yl]amino]-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-[[(2R)-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-oxopentanoic acid | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0007 | uM |
| (4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(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-[[(2R)-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]-4-carboxybutanoyl]amino]-6-aminohexanoyl]amino]-4-carboxybutanoyl]amino]-4-carboxybutanoyl]amino]propanoyl]amino]-5-[[(2S)-4-amino-1-[[(2S)-4-amino-1-[[(2S)-6-amino-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]-1-oxohexan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-5-oxopentanoic acid | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0009 | uM |
| (4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(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-[[(2R)-2-acetamido-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]-4-carboxybutanoyl]amino]-6-aminohexanoyl]amino]-4-carboxybutanoyl]amino]-5-[[(2S)-1-[[(3S,6R,9S,18S)-18-[[(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]carbamoyl]-3,6-bis(2-amino-2-oxoethyl)-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoic acid | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0011 | 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 | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0012 | uM |
| (3S,5S)-3-[[(2R)-2-[(2S)-2-[[(2S,3S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidine-1-carbonyl]amino]-5-[[(2S)-2,4-diamino-4-oxobutanoyl]amino]-4-oxoheptanedioic acid | 223372: Binding affinity of the receptor h-CRF2-alpha with peptidic agonists | ki | 0.0013 | 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-[[(2R)-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-[[(3R,6S,9S,18R)-18-[[(2S)-1-[[(2S)-4-amino-1-[[(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]amino]-1,4-dioxobutan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]-3,6-bis(3-amino-3-oxopropyl)-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-5-oxopentanoic acid | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0013 | uM |
| (4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(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-[[(2R)-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]-4-carboxybutanoyl]amino]-6-aminohexanoyl]amino]-4-carboxybutanoyl]amino]-5-[[(2S)-1-[[(3S,6R,9S,18S)-18-[[(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]carbamoyl]-3,6-bis(2-amino-2-oxoethyl)-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoic acid | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0013 | uM |
| (4S)-5-[[(2S)-6-amino-1-[[(2S)-5-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-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]amino]-1,4-dioxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-[[(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)-2-[[(2S,3S)-2-[[(2S)-1-[(2R)-1-[2-[[(2S)-2,5-diamino-5-oxopentanoyl]amino]acetyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-3-methylpentanoyl]amino]-3-hydroxypropanoyl]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]-5-oxopentanoic acid | 223371: Activity of peptidic agonists on h-CRF2-alpha receptor using agonist-stimulated adenylate cyclase assay | ec50 | 0.0014 | 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 | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0016 | uM |
| (4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(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-[[(2R)-2-acetamido-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]-4-carboxybutanoyl]amino]-6-aminohexanoyl]amino]-4-carboxybutanoyl]amino]-4-carboxybutanoyl]amino]propanoyl]amino]-5-[[(2S)-4-amino-1-[[(2S)-4-amino-1-[[(2S)-6-amino-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]-1-oxohexan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-5-oxopentanoic acid | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0019 | uM |
| (4S)-5-[[(3R,6S,9S,18R)-18-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S,3S)-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]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]carbamoyl]-3-methyl-6-(2-methylpropyl)-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-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-[[(2R)-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 | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0049 | uM |
| (4S)-5-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(3R,6S,9S,18R)-18-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S,3S)-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]amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]-6-(3-amino-3-oxopropyl)-3-methyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-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-[[(2R)-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 | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0050 | uM |
| (4S)-5-[[(2S)-5-amino-1-[[(2S)-1-[[(3S,6R,18S)-18-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S,3S)-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]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]carbamoyl]-3,6-bis(3-amino-3-oxopropyl)-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-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-[[(2R)-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 | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0055 | uM |
| (2S,3S)-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-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-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-1-[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-3-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-4-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]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]-4-methylsulfanylbutanoyl]amino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]propanoyl]amino]-4-carboxybutanoyl]amino]-5-oxopentanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-oxopentanoyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-4-carboxybutanoyl]amino]-3-methylpentanoyl]amino]-3-methylpentanoic acid | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0062 | uM |
| (4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-5-amino-2-[[(2S,5R,8R,17S)-2-(3-amino-3-oxopropyl)-17-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-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-(2-methylpropyl)-3,6,14,18-tetraoxo-1,4,7,13-tetrazacyclooctadecane-8-carbonyl]amino]-5-oxopentanoyl]amino]hexanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]amino]-5-[[(2S,3S)-1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-5-oxopentanoic acid | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0062 | uM |
| (4S)-5-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-5-amino-1-[[(2S)-1-[[(3R,6S,9S,18R)-18-[[(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]carbamoyl]-3-(2-amino-2-oxoethyl)-6-(hydroxymethyl)-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-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 | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0100 | uM |
| (4S)-5-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2R)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-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]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-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-[[(2R)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-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,3S)-2-[[(2S)-1-[(2R)-1-[(2R)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-4-carboxybutanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-3-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-4-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]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]amino]-4-methylsulfanylbutanoyl]amino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]propanoyl]amino]-5-oxopentanoic acid | 223372: Binding affinity of the receptor h-CRF2-alpha with peptidic agonists | ki | 0.0122 | uM |
| (4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(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-[[(2R)-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]-4-carboxybutanoyl]amino]-6-aminohexanoyl]amino]-4-carboxybutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-4-amino-1-[[(3R,6S,9S,18R)-18-[[(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]carbamoyl]-3,6-bis(2-methylpropyl)-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,4-dioxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoic acid | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0178 | uM |
| 5-[[cyclopropylmethyl(propyl)amino]methyl]-N-(2,4,6-trichlorophenyl)-4-(trifluoromethyl)-1,3-thiazol-2-amine | 54123: Effective concentration against Corticotropin releasing factor receptor 2 in IMR-32 cells | ec50 | 0.0420 | uM |
| (4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S,5R,8R,17S)-5-(3-amino-3-oxopropyl)-17-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-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]-2-(2-carboxyethyl)-3,6,14,18-tetraoxo-1,4,7,13-tetrazacyclooctadecane-8-carbonyl]amino]propanoyl]amino]-5-oxopentanoyl]amino]-5-oxopentanoyl]amino]propanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]amino]-5-[[(2S,3R)-1-[[(2S,3R)-1-amino-3-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-5-oxopentanoic acid | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0460 | uM |
| (4S)-5-[[(2S)-1-[[(2S)-5-amino-1-[[(3R,6S,9S,18R)-18-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S,3S)-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]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]-3-(3-amino-3-oxopropyl)-6-methyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-carboxy-1-oxobutan-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-[[(2R)-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]-5-oxopentanoic acid | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0600 | uM |
| Corticorelin Ovine Triflutate | 223371: Activity of peptidic agonists on h-CRF2-alpha receptor using agonist-stimulated adenylate cyclase assay | ec50 | 0.0619 | uM |
| (4S)-5-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(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]amino]-1-oxohexan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-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-[[(2R)-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 | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0690 | 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-[[(2R)-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-[[(3S,6R,9S,18S)-18-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-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]carbamoyl]-3-(2-amino-2-oxoethyl)-6-methyl-2,5,8,12-tetraoxo-1,4,7,13-tetrazacyclooctadec-9-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-oxopentanoic acid | 54132: Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand | ic50 | 0.0810 | uM |
CTD chemical–gene interactions
16 total (human), top 16 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| sodium arsenite | increases expression | 1 |
| sauvagine | affects binding, increases activity, increases reaction | 1 |
| S-(1,2-dichlorovinyl)cysteine | affects response to substance, increases expression | 1 |
| CGP 52608 | affects binding, increases reaction | 1 |
| astressin | affects binding, decreases activity | 1 |
| astressin B | affects binding, decreases activity | 1 |
| Resveratrol | affects cotreatment, decreases expression | 1 |
| Arsenic | affects methylation | 1 |
| Atrazine | increases expression | 1 |
| Benzo(a)pyrene | increases methylation | 1 |
| Lipopolysaccharides | affects response to substance, increases expression | 1 |
| Plant Extracts | affects cotreatment, decreases expression | 1 |
| Silicon Dioxide | increases expression | 1 |
| Tetrachlorodibenzodioxin | increases expression | 1 |
| Antirheumatic Agents | increases expression | 1 |
| Endocannabinoids | affects binding, increases activity, increases reaction | 1 |
ChEMBL screening assays
34 unique, capped per target: 21 binding, 13 functional
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1963888 | Functional | PUBCHEM_BIOASSAY: Dose Response confirmation of uHTS hits for small molecule antagonists of the CRF-binding protein and CRF-R2 receptor complex. (Class of assay: confirmatory) | PubChem BioAssay data set |
| CHEMBL1247746 | Binding | Binding affinity to human recombinant CRF2alpha receptor | Spiroindolones, a potent compound class for the treatment of malaria. — Science |
Cellosaurus cell lines
8 cell lines: 4 spontaneously immortalized cell line, 2 transformed cell line, 2 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_C0SG | ACTOne CRHR2 | Transformed cell line | Female |
| CVCL_H416 | CHO-K1/CRF2/Galpha15 | Spontaneously immortalized cell line | Female |
| CVCL_KU98 | cAMP Hunter CHO-K1 CRHR2 Gs | Spontaneously immortalized cell line | Female |
| CVCL_KW75 | PathHunter CHO-K1 CRHR2 beta-arrestin | Spontaneously immortalized cell line | Female |
| CVCL_LA09 | PathHunter U2OS CRHR2 Activated GPCR Internalization | Cancer cell line | Female |
| CVCL_YK10 | HEK293 CRHR2 HiTSeeker | Transformed cell line | Female |
| CVCL_YK42 | U2OS CRHR2 cAMP-Nomad | Cancer cell line | Female |
| CVCL_ZK51 | GeneBLAzer CRHR2-CRE-bla CHO-K1 | Spontaneously immortalized cell line | Female |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.