ChEMBL ligand: CHEMBL9946 (CP-154526)
CRF1 receptor/Corticotropin releasing factor receptor 1 in Human [ChEMBL: CHEMBL1800] [GtoPdb: 212] [UniProtKB: P34998] CRF1 receptor/Corticotropin releasing factor receptor 1 in Rat [ChEMBL: CHEMBL4649] [GtoPdb: 212] [UniProtKB: P35353] There should be some charts here, you may need to enable JavaScript!
CRF2 receptor/Corticotropin releasing factor receptor 2 in Rat [ChEMBL: CHEMBL3581] [GtoPdb: 213] [UniProtKB: P47866] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
CRF1 receptor/Corticotropin releasing factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1800] [GtoPdb: 212] [UniProtKB: P34998]
ChEMBL	Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells	B	7.25	pKi	56	nM	Ki	Bioorg Med Chem Lett (1998) 8: 2067-2070 [PMID:9873487]
ChEMBL	Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells	B	8.43	pKi	3.7	nM	Ki	Bioorg Med Chem Lett (2005) 15: 3870-3873 [PMID:15990298]
ChEMBL	Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.	B	8.43	pKi	3.7	nM	Ki	Bioorg Med Chem Lett (2003) 13: 3997-4000 [PMID:14592493]
ChEMBL	Antagonist activity at human CRF-1 receptor	F	8.52	pKi	3	nM	Ki	J Med Chem (2011) 54: 4187-4206 [PMID:21618986]
ChEMBL	Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells	B	8.52	pKi	3	nM	Ki	Bioorg Med Chem Lett (2008) 18: 4486-4490 [PMID:18672365]
ChEMBL	Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells	B	8.57	pKi	2.7	nM	Ki	Bioorg Med Chem Lett (2008) 18: 891-896 [PMID:18180159]
ChEMBL	Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells	B	8.57	pKi	2.7	nM	Ki	Bioorg Med Chem Lett (1999) 9: 1057-1062 [PMID:10230640]
ChEMBL	Antagonistic activity for Corticotropin releasing factor receptor 1	F	8.57	pKi	2.7	nM	Ki	Bioorg Med Chem Lett (1999) 9: 1063-1066 [PMID:10230641]
ChEMBL	Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells	B	8.57	pKi	2.7	nM	Ki	Bioorg Med Chem Lett (2002) 12: 2133-2136 [PMID:12127521]
ChEMBL	Binding affinity against [125I]-Try0-o-Corticotropin-releasing Factor to Corticotropin releasing hormone receptor 1 from ovine	B	8.57	pKi	2.7	nM	Ki	J Med Chem (1997) 40: 1749-1754 [PMID:9171885]
ChEMBL	Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells	B	8.57	pKi	2.7	nM	Ki	Bioorg Med Chem Lett (2005) 15: 3870-3873 [PMID:15990298]
ChEMBL	Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells	B	8.79	pKi	1.61	nM	Ki	J Med Chem (1999) 42: 833-848 [PMID:10072681]
ChEMBL	Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane	B	7.8	pIC50	15.85	nM	IC50	Bioorg Med Chem Lett (2007) 17: 5218-5221 [PMID:17629700]
ChEMBL	Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells	B	7.96	pIC50	11	nM	IC50	Bioorg Med Chem Lett (2011) 21: 2365-2371 [PMID:21414781]
CRF1 receptor/Corticotropin releasing factor receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4649] [GtoPdb: 212] [UniProtKB: P35353]
ChEMBL	Inhibition of binding of 70 pM [125I]-Try0-o-Corticotropin-releasing Factor (CFR) to Corticotropin releasing hormone receptor 1 in Rat brain membrane	B	8.26	pIC50	5.5	nM	IC50	J Med Chem (1997) 40: 1749-1754 [PMID:9171885]
GtoPdb	-	-	10.41	pIC50	0.04	nM	IC50	Eur J Pharmacol (1996) 309: 195-200 [PMID:8874139]
CRF2 receptor/Corticotropin releasing factor receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3581] [GtoPdb: 213] [UniProtKB: P47866]
ChEMBL	Inhibition of binding of [125I]-Tyr0-sauvagine to Corticotropin releasing hormone receptor 2 (CRF2)	B	5	pKi	>10000	nM	Ki	J Med Chem (1997) 40: 1749-1754 [PMID:9171885]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]