ChEMBL ligand: CHEMBL482950 (Bms562086, BMS-562086, CRF1 ANTAGONIST, Dpc-a69448, Pexacerfont)
A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] There should be some charts here, you may need to enable JavaScript!
Corticotropin-releasing factor-binding protein in Human [ChEMBL: CHEMBL5930] [UniProtKB: P24387] There should be some charts here, you may need to enable JavaScript!
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 Human [ChEMBL: CHEMBL4069] [GtoPdb: 213] [UniProtKB: Q13324] There should be some charts here, you may need to enable JavaScript!
NK2 receptor/Neurokinin 2 receptor in Human [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452] 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
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL	Binding affinity to rat adenosine A1 receptor expressed in CHO cells	B	5.58	pKi	2660	nM	Ki	J Med Chem (2009) 52: 3084-3092 [PMID:19361209]
Corticotropin-releasing factor-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5930] [UniProtKB: P24387]
ChEMBL	Binding affinity to human recombinant CRF binding protein	B	6	pIC50	>1000	nM	IC50	J Med Chem (2009) 52: 3084-3092 [PMID:19361209]
ChEMBL	Binding affinity to CRF-binding protein (unknown origin)	B	6	pIC50	>1000	nM	IC50	Drug Metab Dispos (2012) 40: 1093-1103 [PMID:22381334]
CRF1 receptor/Corticotropin releasing factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1800] [GtoPdb: 212] [UniProtKB: P34998]
ChEMBL	Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by compound washout for 2 hrs and subsequent addition of [125I]-CRF measured after 1 hr by liquid scintillation counting method	B	5	pIC50	>10000	nM	IC50	Bioorg Med Chem (2017) 25: 1556-1570 [PMID:28174066]
ChEMBL	Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition measured after 1 hr by liquid scintillation counting method	B	6.47	pIC50	340	nM	IC50	Bioorg Med Chem (2017) 25: 1556-1570 [PMID:28174066]
GtoPdb	Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes.	-	6.47	pIC50	340	nM	IC50	Bioorg Med Chem (2017) 25: 1556-1570 [PMID:28174066]
ChEMBL	Antagonist activity at human CRF1 receptor	B	8.21	pIC50	6.1	nM	IC50	Drug Metab Dispos (2012) 40: 1093-1103 [PMID:22381334]
ChEMBL	Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in human IMR32 cells	B	8.35	pIC50	4.5	nM	IC50	J Med Chem (2009) 52: 3084-3092 [PMID:19361209]
CRF1 receptor/Corticotropin releasing factor receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4649] [GtoPdb: 212] [UniProtKB: P35353]
ChEMBL	Antagonist activity at CRF1 receptor in rat pituitary cells assessed as inhibition of CRF-mediated ACTH production	F	6.89	pIC50	129	nM	IC50	J Med Chem (2009) 52: 3084-3092 [PMID:19361209]
GtoPdb	Antagonism of CRF-mediated ACTH production in rat pituitary cells.	-	6.89	pIC50	129	nM	IC50	Bioorg Med Chem (2017) 25: 1556-1570 [PMID:28174066]
ChEMBL	Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting	B	8.21	pIC50	6.1	nM	IC50	J Med Chem (2009) 52: 3084-3092 [PMID:19361209]
ChEMBL	Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting	B	8.21	pIC50	6.1	nM	IC50	J Med Chem (2011) 54: 4187-4206 [PMID:21618986]
CRF2 receptor/Corticotropin releasing factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4069] [GtoPdb: 213] [UniProtKB: Q13324]
ChEMBL	Displacement of [125I]Tyr0-sauvagine from CRF2beta receptor expressed in pig choroid plexus membrane	B	6	pIC50	>1000	nM	IC50	J Med Chem (2009) 52: 3084-3092 [PMID:19361209]
NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
ChEMBL	Binding affinity to human neurokinin 2 receptor	B	5.31	pIC50	4900	nM	IC50	J Med Chem (2009) 52: 3084-3092 [PMID:19361209]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]