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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  • 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 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 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 activation of K+ currents B 4.51 pEC50 31000 nM EC50 J Med Chem (2007) 50: 2117-2126 [PMID:17425298]
ChEMBL Activation of Kir6.2/SUR1 (unknown origin) channel opening expressed in human T-REx-293 cells by thallium flux assay B 4.52 pEC50 30000 nM EC50 Bioorg Med Chem Lett (2023) 87: 129256-129256 [PMID:36966977]
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 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]