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

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ChEMBL ligand: CHEMBL3304485 (AZD-1722, Tenapanor)
  • Sodium/hydrogen exchanger 3 in Human [ChEMBL: CHEMBL3273] [GtoPdb: 950] [UniProtKB: P48764]
  • Sodium/hydrogen exchanger 3 in Rat [ChEMBL: CHEMBL3879842] [GtoPdb: 950] [UniProtKB: P26433]
  • This target only has 0 pki data point
  • 0
1 CHEMBL3304485_lig_chart_1 Sodium/hydrogen exchanger 3 HumanRat
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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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]