repaglinide [Ligand Id: 6841] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1272 (A10BX02, AG-EE 623 ZW, AG-EE-623ZW, AG-EE-623-ZW, AGEE-623ZW, Enyglid, Novonorm, NSC-759893, Prandin, Repaglinide)
  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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  • ATP-binding cassette, sub-family C (CFTR/MRP), member 8/Sulfonylurea receptor 1 in Human [ChEMBL: CHEMBL2071] [GtoPdb: 2594] [UniProtKB: Q09428]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
ChEMBL Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy B 5.04 pIC50 9200 nM IC50 J Med Chem (2008) 51: 5932-5942 [PMID:18788725]
ATP-binding cassette, sub-family C (CFTR/MRP), member 8/Sulfonylurea receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2071] [GtoPdb: 2594] [UniProtKB: Q09428]
ChEMBL Displacement of [3H]glibenclamide from COS-1 cells expressing Sulfonylurea receptor 1 (SUR-1) B 7.3 pKd 50 nM Kd Bioorg Med Chem Lett (2004) 14: 5205-5209 [PMID:15380228]
GtoPdb - - 6.97 pIC50 106 nM IC50 Bioorg Med Chem Lett (2004) 14: 5205-9 [PMID:15380228]
ChEMBL In vitro displacement of [3H]glibenclamide (IC50=0.61) from COS-1 cells expressing Sulfonylurea receptor 1 (SUR-1) B 6.97 pIC50 106 nM IC50 Bioorg Med Chem Lett (2004) 14: 5205-5209 [PMID:15380228]

ChEMBL data shown on this page come from version 32:

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]