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 (2016) |
| ChEMBL | Inhibition of human NHE3 expressed in opossum kidney cells assessed as reduction in Na-HEPES buffer-mediated pH recovery in presence of NEH1 inhibitor ethyl isopropyl amiloride by BCECF-AM dye based fluorescence assay | B | 9.3 | pIC50 | 0.5 | nM | IC50 | ACS Med Chem Lett (2022) 13: 1043-1051 [PMID:35859876] |
| 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 expressed in opossum kidney cells assessed as reduction in Na-HEPES buffer-mediated pH recovery in presence of NEH1 inhibitor ethyl isopropyl amiloride by BCECF-AM dye based fluorescence assay | B | 7.8 | pIC50 | 15.85 | nM | IC50 | ACS Med Chem Lett (2022) 13: 1043-1051 [PMID:35859876] |
| 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 (2016) |
ChEMBL data shown on this page come from version 34:
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]
