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ChEMBL ligand: CHEMBL9946 (CP-154526) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 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]