devazepide [Ligand Id: 878] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL39263 (Rac-Devazepide) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CCK1 receptor/Cholecystokinin A receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1901] [GtoPdb: 76] [UniProtKB: P32238] | ||||||||
| ChEMBL | Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK1 receptor expressed in COS-7 cells after 60 mins by gamma counting | B | 7.98 | pKi | 10.4 | nM | Ki | J Med Chem (2011) 54: 5769-5785 [PMID:21728335] |
| CCK1 receptor/Cholecystokinin A receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2871] [GtoPdb: 76] [UniProtKB: P30551] | ||||||||
| ChEMBL | Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue | B | 9.1 | pIC50 | 0.8 | nM | IC50 | J Med Chem (1988) 31: 2235-2246 [PMID:2848124] |
| ChEMBL | Binding affinity against cholecystokinin type A receptor of rat pancreas | B | 9.1 | pIC50 | 0.79 | nM | IC50 | J Med Chem (1994) 37: 3639-3654 [PMID:7932591] |
| GtoPdb | - | - | 9.72 | pIC50 | 0.19 | nM | IC50 | Proc Natl Acad Sci USA (1990) 87: 6728-32 [PMID:1975695] |
| CCK2 receptor/Cholecystokinin B receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL298] [GtoPdb: 77] [UniProtKB: P32239] | ||||||||
| ChEMBL | Displacement of [125I]BH-(Thr,-Nle)-CCK-9 from human CCK2 receptor expressed in COS-7 cells after 60 mins by gamma counting | B | 6.77 | pKi | 169 | nM | Ki | J Med Chem (2011) 54: 5769-5785 [PMID:21728335] |
| ChEMBL | Half-maximal inhibition of [125I]gastrin binding to guinea pig gastric glands | B | 6.14 | pIC50 | 720 | nM | IC50 | J Med Chem (1988) 31: 2235-2246 [PMID:2848124] |
| GtoPdb | - | - | 6.8 | pIC50 | - | - | - | J Biol Chem (1993) 268: 8164-9 [PMID:7681836] |
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]
