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 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]
