VU0240551 [Ligand Id: 4665] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1491962
  • Basolateral Na-K-Cl symporter/Solute carrier family 12 member 2 in Human [ChEMBL: CHEMBL1615383] [GtoPdb: 969] [UniProtKB: P55011]
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  • K-Cl cotransporter 2/Solute carrier family 12 member 5 in Human [ChEMBL: CHEMBL1615384] [GtoPdb: 972] [UniProtKB: Q9H2X9]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Basolateral Na-K-Cl symporter/Solute carrier family 12 member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1615383] [GtoPdb: 969] [UniProtKB: P55011]
ChEMBL Antagonist activity at NKKC1 expressed in human HEK293 cells assessed as [86Rb] uptake after 30 mins by scintillation counting F 4.3 pIC50 >50000 nM IC50 Bioorg Med Chem Lett (2012) 22: 4532-4535 [PMID:22727639]
K-Cl cotransporter 2/Solute carrier family 12 member 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1615384] [GtoPdb: 972] [UniProtKB: Q9H2X9]
ChEMBL Antagonist activity at KCC2 expressed in human HEK293 cells assessed as decrease in Tl-stimulated fluorescence increase after 8 mins by fluorescence analysis F 6.25 pIC50 568 nM IC50 Bioorg Med Chem Lett (2012) 22: 4532-4535 [PMID:22727639]
GtoPdb - - 6.25 pIC50 560 nM IC50 Proc Natl Acad Sci USA (2009) 106: 5383-8 [PMID:19279215]

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]