amiloride [Ligand Id: 2421] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL945 (Amiloride, Hydro-Ride, Midamor)
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
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  • ASIC3/Amiloride-sensitive cation channel 3 in Human [ChEMBL: CHEMBL5368] [GtoPdb: 686] [UniProtKB: Q9UHC3]
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  • ENaC α/Amiloride-sensitive sodium channel alpha-subunit in Human [ChEMBL: CHEMBL1791] [GtoPdb: 738] [UniProtKB: P37088]
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  • amine oxidase copper containing 3/Amine oxidase, copper containing in Rat [ChEMBL: CHEMBL4592] [GtoPdb: 2767] [UniProtKB: O08590]
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  • Sodium/hydrogen exchanger in Amphiuma tridactylum [ChEMBL: CHEMBL5418] [UniProtKB: Q9W6Q1]
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  • Sodium/hydrogen exchanger 2 in Rabbit [ChEMBL: CHEMBL3770] [UniProtKB: P50482]
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  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
  • Organic cation transporter 1/Solute carrier family 22 member 1 in Rat [ChEMBL: CHEMBL2073670] [GtoPdb: 1019] [UniProtKB: Q63089]
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  • Organic cation transporter 2/Solute carrier family 22 member 2 in Rat [ChEMBL: CHEMBL1770032] [GtoPdb: 1020] [UniProtKB: Q9R0W2]
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  • plasminogen activator, urokinase/Urokinase-type plasminogen activator in Human [ChEMBL: CHEMBL3286] [GtoPdb: 2393] [UniProtKB: P00749]
  • plasminogen activator, urokinase/Urokinase-type plasminogen activator in Mouse [ChEMBL: CHEMBL1075311] [GtoPdb: 2393] [UniProtKB: P06869]
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  • TRPA1 in Mouse [GtoPdb: 485] [UniProtKB: Q8BLA8]
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  • TRPC6 in Mouse [GtoPdb: 491] [UniProtKB: Q61143]
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  • TRPP2 in Human [GtoPdb: 505] [UniProtKB: Q9P0L9]
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  • ASIC2 in Human [GtoPdb: 685] [UniProtKB: Q16515]
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  • ENaCαβγ in Human [GtoPdb: 742]
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  • Sodium/hydrogen exchanger 2 in Rabbit [GtoPdb: 949]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ASIC1 in Human [GtoPdb: 684] [UniProtKB: P78348]
GtoPdb - - 4.68 pIC50 21000 nM IC50
GtoPdb - - 5 pIC50 10000 nM IC50
ASIC1/Acid-sensing ion channel 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3562170] [GtoPdb: 684] [UniProtKB: P55926]
ChEMBL Inhibition of ASIC1 in Sprague-Dawley rat articular chondrocytes assessed as decrease in acid-induced intracellular calcium level by Fluo-3AM dye based laser scanning confocal microscopy B 4.52 pIC50 30200 nM IC50 Bioorg Med Chem (2018) 26: 3158-3165 [PMID:29699911]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Binding affinity for HA-tagged wild type human Adenosine A2A receptor (WT) using [3H]CGS-21680 as radioligand expressed in COS-7 cells B 4.92 pKi 12000 nM Ki J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Binding affinity for HA-tagged mutant human Adenosine A2A receptor (V84L), using [3H]CGS-21680 as radioligand expressed in COS-7 cells B 4.94 pKi 11600 nM Ki J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Binding affinity for HA-tagged mutant human Adenosine A2A receptor (H250N) using [3H]-CGS-21,680 as radioligand expressed in COS-7 cells B 5.48 pKi 3280 nM Ki J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
ASIC3/Amiloride-sensitive cation channel 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5368] [GtoPdb: 686] [UniProtKB: Q9UHC3]
GtoPdb - - 4.8 pIC50 16000 nM IC50
ChEMBL Inhibition of ASIC3 assessed as inhibition of peak current by patch clamp electrophysiology B 5.36 pIC50 4400 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 2514-2518 [PMID:19339181]
ENaC α/Amiloride-sensitive sodium channel alpha-subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1791] [GtoPdb: 738] [UniProtKB: P37088]
ChEMBL Inhibition of dog bronchi prototypical epithelial sodium channel by electrophysiological assay B 6.11 pIC50 776 nM IC50 J. Med. Chem. (2006) 49: 4098-4115 [PMID:16821771]
amine oxidase copper containing 3/Amine oxidase, copper containing in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4592] [GtoPdb: 2767] [UniProtKB: O08590]
ChEMBL Inhibitory activity against porcine kidney amine oxidase B 5 pKi 10000 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 2565-2568 [PMID:11551750]
Monoamine oxidase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397]
ChEMBL DRUGMATRIX: Monoamine Oxidase MAO-A enzyme inhibition (substrate: Kynuramine) B 5.41 pIC50 3909 nM IC50 DrugMatrix in vitro pharmacology data
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 4.01 pIC50 98000 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 4.22 pIC50 60000 nM IC50 J. Biol. Chem. (2007) 282: 19716-19727 [PMID:17493937]
Sodium/hydrogen exchanger 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2577] [GtoPdb: 948] [UniProtKB: P26431]
GtoPdb - - 6 pKi 1000 nM Ki Eur J Med Chem (2003) 38: 547-54 [PMID:12832126]
ChEMBL Inhibition of rat NHE1 expressed in chinese hamster AP1 cells assessed as inhibition of acid-induced 22Na+ influx by liquid scintillation spectroscopy B 6 pKi 1000 nM Ki WO-2014169094-A2. NHE3-binding compounds and methods for inhibiting phosphate transport (2014)
ChEMBL Inhibition of rat NHE-1 B 6 pKi 1000 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 6 pIC50 1000 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 pKi 1000 nM Ki WO-2014169094-A2. NHE3-binding compounds and methods for inhibiting phosphate transport (2014)
ChEMBL Inhibition of rabbit NHE-2 B 6 pKi 1000 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 pIC50 1000 nM IC50 US20160067242A1. 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 - - 4 pKi >100000 nM Ki Eur J Med Chem (2003) 38: 547-54 [PMID:12832126]
ChEMBL Inhibition of rat NHE3 expressed in chinese hamster AP1 cells assessed as inhibition of acid-induced 22NA+ influx by liquid scintillation spectroscopy B 4 pKi >100000 nM Ki WO-2014169094-A2. NHE3-binding compounds and methods for inhibiting phosphate transport (2014)
ChEMBL Inhibition of rat NHE-3 B 4 pKi >100000 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 4 pIC50 >100000 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 4.68 pKi 21000 nM Ki WO-2014169094-A2. NHE3-binding compounds and methods for inhibiting phosphate transport (2014)
ChEMBL Inhibition of NHE-5 (unknown origin) B 4.68 pKi 21000 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)
GtoPdb - - 4.68 pKi 21000 nM Ki Eur J Med Chem (2003) 38: 547-54 [PMID:12832126]
ChEMBL Inhibition of NHE5 (unknown origin) B 4.68 pIC50 21000 nM IC50 US20160067242A1. Nhe3-binding compounds and methods for inhibiting phosphate transport (null)
Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
ChEMBL Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy B 4.24 pIC50 57000 nM IC50 J. Med. Chem. (2008) 51: 5932-5942 [PMID:18788725]
Organic cation transporter 1/Solute carrier family 22 member 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073670] [GtoPdb: 1019] [UniProtKB: Q63089]
ChEMBL TP_TRANSPORTER: inhibition of TEA uptake in OCT1-expressing MDCK cells F 5.16 pKi 6900 nM Ki Pharm. Res. (2001) 18: 1528-1534 [PMID:11758759]
Organic cation transporter 2/Solute carrier family 22 member 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1770032] [GtoPdb: 1020] [UniProtKB: Q9R0W2]
ChEMBL TP_TRANSPORTER: inhibition of TEA uptake in OCT2-expressing MDCK cells F 5.33 pKi 4700 nM Ki Pharm. Res. (2001) 18: 1528-1534 [PMID:11758759]
plasminogen activator, urokinase/Urokinase-type plasminogen activator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3286] [GtoPdb: 2393] [UniProtKB: P00749]
ChEMBL Inhibition of uPA (unknown origin) using L-pyroglutamyl-glycyl-L-arginine-p-nitro-anilide as susbtrate by Lineweaver-Burk plot analysis B 5.15 pKi 7000 nM Ki J Med Chem (2018) 61: 8299-8320 [PMID:30130401]
ChEMBL Inhibition of urokinase B 5.6 pKi 2511.89 nM Ki J. Med. Chem. (2009) 52: 3159-3165 [PMID:19385614]
ChEMBL Inhibition of human kidney uPA using Z-Gly-Gly-Arg-AMC as substrate measured over 15 mins by fluorescence assay B 5.61 pKi 2433 nM Ki J Med Chem (2018) 61: 8299-8320 [PMID:30130401]
ChEMBL Inhibition of human uPA using pyro-Glu-Gly-Arg-pNA as substrate assessed as para-nitroaniline release from substrate measured for 5 mins by spectrophotometric assay B 4.92 pIC50 11980 nM IC50 J. Med. Chem. (2015) 58: 9238-9257 [PMID:26575094]
ChEMBL Inhibitory activity against Urokinase-type plasminogen activator B 5.15 pIC50 7000 nM IC50 J. Med. Chem. (2000) 43: 3862-3866 [PMID:11052791]
ChEMBL Inhibition of urokinase-type plasminogen activator using Glt-Gly-Arg-AMC as substrate by spectrofluorometry B 5.15 pIC50 7000 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 2635-2639 [PMID:22366654]
plasminogen activator, urokinase/Urokinase-type plasminogen activator in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075311] [GtoPdb: 2393] [UniProtKB: P06869]
ChEMBL Inhibition of mouse uPA using Z-Gly-Gly-Arg-AMC as substrate after 15 mins by fluorescence assay B 5.64 pKi 2313 nM Ki J Med Chem (2018) 61: 8299-8320 [PMID:30130401]
TRPA1 in Mouse [GtoPdb: 485] [UniProtKB: Q8BLA8]
GtoPdb - - 3.3 pIC50 - - - J. Neurosci. (2005) 25: 4052-61 [PMID:15843607]
TRPC6 in Mouse [GtoPdb: 491] [UniProtKB: Q61143]
GtoPdb - - 3.9 pIC50 129000 nM IC50 Circ. Res. (2001) 88: 325-32 [PMID:11179201]
TRPP2 in Human [GtoPdb: 505] [UniProtKB: Q9P0L9]
GtoPdb - - 3.8 pIC50 143000 nM IC50
ASIC2 in Human [GtoPdb: 685] [UniProtKB: Q16515]
GtoPdb - - 4.6 pIC50 28000 nM IC50
ENaCαβγ in Human [GtoPdb: 742]
GtoPdb - - 7 pIC50 100 nM IC50
Sodium/hydrogen exchanger 2 in Rabbit [GtoPdb: 949]
GtoPdb - - 7.1 pKi 80 nM Ki Eur J Med Chem (2003) 38: 547-54 [PMID:12832126]

ChEMBL data shown on this page come from version 26:

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]