CP 154,526 [Ligand Id: 3495] activity data from GtoPdb and ChEMBL

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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]
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  • CRF2 receptor/Corticotropin releasing factor receptor 2 in Rat [ChEMBL: CHEMBL3581] [GtoPdb: 213] [UniProtKB: P47866]
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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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]