diazoxide [Ligand Id: 2409] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL181 (Diazoxide, Diazoxidum, Eudemine, Eudemine injection, Eudimine, Hyperstat, Hypertonalum, Mutabase, NSC-64198, NSC-76130, Proglycem, SCH 6783, SCH-6783, SRG 95213, SRG-95213) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ATP-binding cassette, sub-family C (CFTR/MRP), member 8/Kir6.2/Sulfonylurea receptor 1, Kir6.2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096972] [GtoPdb: 2594, 442] [UniProtKB: Q09428, Q14654] | ||||||||
| ChEMBL | Repolarization of HEK293 cells expressing Kir6.2/SUR1 KATP channels | F | 4.48 | pEC50 | 33000 | nM | EC50 | J Med Chem (2006) 49: 4127-4139 [PMID:16821773] |
| ChEMBL | Activity at Kir6.2/SUR1 KATP channels expressed in HEK293 cells assessed as repolarization of tolbutamide-induced membrane depolarization | B | 4.48 | pEC50 | 33000 | nM | EC50 | J Med Chem (2007) 50: 2117-2126 [PMID:17425298] |
| ChEMBL | Activity at Kir6.2/SUR1 KATP channels expressed in HEK293 cells assessed as activation of K+ currents | B | 4.51 | pEC50 | 31000 | nM | EC50 | J Med Chem (2007) 50: 2117-2126 [PMID:17425298] |
| ChEMBL | Activation of human recombinant SUR1/Kir6.2 channel expressed in HEK293 cells assessed as increase in ionic current by whole cell patch clamp assay | B | 4.63 | pEC50 | 23500 | nM | EC50 | J Med Chem (2010) 53: 147-154 [PMID:19919106] |
| ChEMBL | Maximum activation of human KATP (SUR1/Kir6.2) channel expressed in Xenopus oocytes | F | 5.06 | pEC50 | 8800 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 813-816 [PMID:14741296] |
| ChEMBL | Inhibition of Beta-cell KATP channel | F | 5.06 | pEC50 | 8800 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 2977-2980 [PMID:12270187] |
| ATP-binding cassette, sub-family C (CFTR/MRP), member 8/Kir6.2 in Mouse [GtoPdb: 2594, 442] [UniProtKB: Q61743] | ||||||||
| GtoPdb | - | - | 4.2 | pEC50 | 63000 | nM | EC50 | Science (1995) 270: 1166-70 [PMID:7502040] |
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]
