diazoxide [Ligand Id: 2409] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL181 (NSC-64198, Mutabase, NSC-76130, SCH 6783, SCH-6783, SRG 95213, Eudemine, Diazoxide, SRG-95213, Eudimine, Hyperstat, Proglycem)
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  • ATP-binding cassette, sub-family C (CFTR/MRP), member 8/Kir6.2/Sulfonylurea receptor 1, Kir6.2 in Human [ChEMBL: CHEMBL2096972] [GtoPdb: 2594442] [UniProtKB: Q09428Q14654]
  • ATP-binding cassette, sub-family C (CFTR/MRP), member 8/Kir6.2 in Mouse [GtoPdb: 2594442] [UniProtKB: Q61743]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Nicotinamide phosphoribosyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1744525] [UniProtKB: P43490]
ChEMBL Binding affinity to NAMPT (2 to 491) (unknown origin) by surface plasmon resonance analysis B 3.64 pKd 230000 nM Kd J. Med. Chem. (2014) 57: 770-792 [PMID:24405419]
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: 2594442] [UniProtKB: Q09428Q14654]
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: 2594442] [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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]