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

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ChEMBL ligand: CHEMBL1272 (A10BX02, AG-EE 623 ZW, AG-EE-623-ZW, AG-EE-623ZW, AGEE-623ZW, Enyglid, Novonorm, NSC-759893, Prandin, Repaglinida, Repaglinide, Repaglinide accord, Repaglinide component of prandimet, Repaglinide krka, Repaglinide teva)
  • ATP-binding cassette, sub-family C (CFTR/MRP), member 8/ATP-binding cassette sub-family C member 8 in Human [ChEMBL: CHEMBL2071] [GtoPdb: 2594] [UniProtKB: Q09428]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
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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/ATP-binding cassette sub-family C member 8 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]
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]

ChEMBL data shown on this page come from version 36:

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]