ethylisopropylamiloride [Ligand Id: 4186] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL517986
There should be some charts here, you may need to enable JavaScript!
  • Sodium/hydrogen exchanger in Amphiuma tridactylum [ChEMBL: CHEMBL5418] [UniProtKB: Q9W6Q1]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • α2A-adrenoceptor in Human [GtoPdb: 25] [UniProtKB: P08913]
There should be some charts here, you may need to enable JavaScript!
  • TRPP2 in Human [GtoPdb: 505] [UniProtKB: Q9P0L9]
There should be some charts here, you may need to enable JavaScript!
  • ASIC1 in Human [GtoPdb: 684] [UniProtKB: P78348]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5.2 pIC50 6309.57 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 infected in RBCs by firefly luciferase reporter gene assay F 6.08 pIC50 825 nM IC50 Antimicrob. Agents Chemother. (2010) 54: 3597-3604 [PMID:20547797]
Sodium/hydrogen exchanger in Amphiuma tridactylum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5418] [UniProtKB: Q9W6Q1]
ChEMBL Inhibition of Amphiuma tridactylum wild type NHE1 expressed in chinese hamster AP1 cells assessed as intracellular pHi recovery by ammonium chloride prepulse protocol B 5.06 pIC50 8700 nM IC50 J. Biol. Chem. (2007) 282: 19716-19727 [PMID:17493937]
Sodium/hydrogen exchanger 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2781] [GtoPdb: 948] [UniProtKB: P19634]
ChEMBL Inhibition of human wild type NHE1 expressed in chinese hamster AP1 cells assessed as intracellular pHi recovery by ammonium chloride prepulse protocol B 6.1 pIC50 800 nM IC50 J. Biol. Chem. (2007) 282: 19716-19727 [PMID:17493937]
Sodium/hydrogen exchanger 1 in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2865] [UniProtKB: P23791]
ChEMBL Inhibition of rabbit NHE1 B 7.7 pKi 20 nM Ki WO-2014169094-A2. NHE3-binding compounds and methods for inhibiting phosphate transport (2014)
ChEMBL Inhibition of rabbit NHE-1 B 7.7 pKi 20 nM Ki US-8541448-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 rabbit NHE1 B 7.7 pIC50 20 nM IC50 US20160067242A1. Nhe3-binding compounds and methods for inhibiting phosphate transport (null)
Sodium/hydrogen exchanger 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2577] [GtoPdb: 948] [UniProtKB: P26431]
ChEMBL Inhibition of rat NHE1 expressed in chinese hamster AP1 cells assessed as inhibition of acid-induced 22Na+ influx by liquid scintillation spectroscopy B 8 pKi 10 nM Ki WO-2014169094-A2. NHE3-binding compounds and methods for inhibiting phosphate transport (2014)
ChEMBL Inhibition of rat NHE-1 B 8 pKi 10 nM Ki US-8541448-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 NHE1 B 8 pIC50 10 nM IC50 US20160067242A1. Nhe3-binding compounds and methods for inhibiting phosphate transport (null)
Sodium/hydrogen exchanger 2 in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3770] [UniProtKB: P50482]
ChEMBL Inhibition of rabbit NHE2 B 6.3 pKi 500 nM Ki WO-2014169094-A2. NHE3-binding compounds and methods for inhibiting phosphate transport (2014)
ChEMBL Inhibition of rabbit NHE-2 B 6.3 pKi 500 nM Ki US-8541448-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 rabbit NHE2 B 6.3 pIC50 500 nM IC50 US20160067242A1. Nhe3-binding compounds and methods for inhibiting phosphate transport (null)
Sodium/hydrogen exchanger 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3886122] [GtoPdb: 949] [UniProtKB: P48763]
ChEMBL Inhibition of rat NHE2 B 7.1 pKi 80 nM Ki WO-2014169094-A2. NHE3-binding compounds and methods for inhibiting phosphate transport (2014)
ChEMBL Inhibition of rat NHE-2 B 7.1 pKi 80 nM Ki US-8541448-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)
Sodium/hydrogen exchanger 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879842] [GtoPdb: 950] [UniProtKB: P26433]
ChEMBL Inhibition of rat NHE3 expressed in chinese hamster AP1 cells assessed as inhibition of acid-induced 22NA+ influx by liquid scintillation spectroscopy B 5.62 pKi 2400 nM Ki WO-2014169094-A2. NHE3-binding compounds and methods for inhibiting phosphate transport (2014)
ChEMBL Inhibition of rat NHE-3 B 5.62 pKi 2400 nM Ki US-8541448-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 B 5.62 pIC50 2400 nM IC50 US20160067242A1. Nhe3-binding compounds and methods for inhibiting phosphate transport (null)
Sodium/hydrogen exchanger 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3058] [GtoPdb: 952] [UniProtKB: Q14940]
ChEMBL Inhibition of full length human C-terminal HA-tagged human NHE5 expressed in chinese hamster AP1 cells assessed as inhibition of acid-induced 22NA+ influx by liquid scintillation spectroscopy B 6.38 pKi 420 nM Ki WO-2014169094-A2. NHE3-binding compounds and methods for inhibiting phosphate transport (2014)
ChEMBL Inhibition of NHE-5 (unknown origin) B 6.38 pKi 420 nM Ki US-8541448-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 NHE5 (unknown origin) B 6.38 pIC50 420 nM IC50 US20160067242A1. Nhe3-binding compounds and methods for inhibiting phosphate transport (null)
α2A-adrenoceptor in Human [GtoPdb: 25] [UniProtKB: P08913]
GtoPdb - - 1.8 pKd - - - Mol. Pharmacol. (1992) 42: 175-9 [PMID:1325028]
TRPP2 in Human [GtoPdb: 505] [UniProtKB: Q9P0L9]
GtoPdb - - 5 pIC50 10500 nM IC50
ASIC1 in Human [GtoPdb: 684] [UniProtKB: P78348]
GtoPdb - - 5 pIC50 10000 nM IC50

ChEMBL data shown on this page come from version 27:

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]