ethylisopropylamiloride [Ligand Id: 4186] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL517986 |
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| 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 | US-20160067242-A1. 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 | US-20160067242-A1. 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 | US-20160067242-A1. 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 | US-20160067242-A1. 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 | US-20160067242-A1. 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 | Nature (1997) 386: 173-7 [PMID:9062189] |
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]
