tenapanor [Ligand Id: 8449] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3304485 (AZD-1722, Khk7791, KHK-7791, Tenapanor)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Sodium/hydrogen exchanger 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3273] [GtoPdb: 950] [UniProtKB: P48764]
ChEMBL Inhibition of human NHE3-mediated sodium-dependant hydrogen ion antiport in Opossum kidney cells preincubated in NH4Cl-HEPES buffer containing BCECF-AM dye followed by washout with ammonium free HEPES and subsequent addition of compound in presence of NHE1 antagonist EIPA by fluorescence assay B 8.3 pIC50 5.01 nM IC50 WO-2014169094-A2. NHE3-binding compounds and methods for inhibiting phosphate transport (2014)
ChEMBL Inhibition of human NHE3 expressed in OK cells assessed as reduction in Na+ dependent H+ antiport in presence of NHE1 inhibitor EIPA by BCECF-AM dye based fluorescence assay B 8.3 pIC50 5.01 nM IC50 US-20160067242-A1. Nhe3-binding compounds and methods for inhibiting phosphate transport (null)
Sodium/hydrogen exchanger 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879842] [GtoPdb: 950] [UniProtKB: P26433]
GtoPdb - - 7 pIC50 <100 nM IC50 US8541448 B2. Compounds and methods for inhibiting NHE-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders. (2013)
ChEMBL Inhibition of rat NHE3-mediated sodium-dependant hydrogen ion antiport in Opossum kidney cells preincubated in NH4Cl-HEPES buffer containing BCECF-AM dye followed by washout with ammonium free HEPES and subsequent addition of compound in presence of NHE1 antagonist EIPA by fluorescence assay B 8.03 pIC50 9.33 nM IC50 WO-2014169094-A2. NHE3-binding compounds and methods for inhibiting phosphate transport (2014)
ChEMBL Inhibition of rat NHE3 expressed in OK cells assessed as reduction in Na+ dependent H+ antiport in presence of NHE1 inhibitor EIPA by BCECF-AM dye based fluorescence assay B 8.03 pIC50 9.33 nM IC50 US-20160067242-A1. Nhe3-binding compounds and methods for inhibiting phosphate transport (null)

ChEMBL data shown on this page come from version 33:

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]