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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 |
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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: 2594, 442] [UniProtKB: Q09428, Q14654] | ||||||||
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: 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 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]