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 (2016) |
| 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 (2016) |
| 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 (2016) |
| 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 (2016) |
| 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 (2016) |
| 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 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]
