amiloride [Ligand Id: 2421] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL945 (Amiclaran, Amiloride, Hydro-Ride, Midamor) |
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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 | Nature (1997) 386: 173-7 [PMID:9062189] |
| 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] |
| Alpha-ketoglutarate-dependent dioxygenase FTO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2331065] [UniProtKB: Q9C0B1] | ||||||||
| ChEMBL | Inhibition of FTO (unknown origin) demethylation activity using m6A7-Broccoli RNA as substrate incubated for 3 mins under shaking condition and measured after 2 hrs by fluorescence based analysis | B | 5.32 | pIC50 | 4740 | nM | IC50 | J Med Chem (2021) 64: 16974-17003 [PMID:34792334] |
| 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 | J Biol Chem (1997) 272: 20975-8 [PMID:9261094] |
| 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] |
| coagulation factor X/Coagulation factor X in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL244] [GtoPdb: 2359] [UniProtKB: P00742] | ||||||||
| ChEMBL | Inhibition of factor Xa (unknown origin) | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126753-126753 [PMID:31679971] |
| coagulation factor XI/Coagulation factor XI in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2820] [GtoPdb: 2360] [UniProtKB: P03951] | ||||||||
| ChEMBL | Inhibition of factor 11a (unknown origin) using chromogenic L-pyroGlu-L-Pro-L-Arg-p-nitroaniline as substrate | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126753-126753 [PMID:31679971] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of recombinant human ERG expressed in CHO cells incubated for 12 mins by whole cell voltage clamp method | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem (2021) 37: 116116-116116 [PMID:33799173] |
| 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 |
| kallikrein B1/Plasma kallikrein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2000] [GtoPdb: 2379] [UniProtKB: P03952] | ||||||||
| ChEMBL | Inhibition of human plasma kallikrein using chromogenic L-pyroGlu-L-Pro-L-Arg-p-nitroaniline as substrate | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126753-126753 [PMID:31679971] |
| plasminogen/Plasminogen in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1801] [GtoPdb: 2394] [UniProtKB: P00747] | ||||||||
| ChEMBL | Inhibition of plasmin (unknown origin) using chromogenic H-D-Ile-L-propyl-L-arginine-p-nitroaniline as substrate | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126753-126753 [PMID:31679971] |
| Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524] | ||||||||
| ChEMBL | Inhibition of recombinant human Nav1.5alpha expressed in HEK293 cells incubated for 10 mins by voltage clamp method | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem (2021) 37: 116116-116116 [PMID:33799173] |
| 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 | 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 | 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 | US-20160067242-A1. Nhe3-binding compounds and methods for inhibiting phosphate transport (2016) |
| 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 | 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 | 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 | US-20160067242-A1. Nhe3-binding compounds and methods for inhibiting phosphate transport (2016) |
| 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] |
| coagulation factor II, thrombin/Thrombin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734] | ||||||||
| ChEMBL | Inhibition of thrombin (unknown origin) using chromogenic H-D-Ile-L-propyl-L-arginine-p-nitroaniline as substrate | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126753-126753 [PMID:31679971] |
| plasminogen activator, tissue type/Tissue-type plasminogen activator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1873] [GtoPdb: 2392] [UniProtKB: P00750] | ||||||||
| ChEMBL | Inhibition of tissue-type plasminogen activator (unknown origin) using chromogenic H-D-Ile-L-propyl-L-arginine-p-nitroaniline as substrate | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126753-126753 [PMID:31679971] |
| 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 uPA (unknown origin) using L-pyroglutamyl-glycyl-L-arginine-p-nitroanilide as substrate by Lineweaver-Burk plot analysis | B | 5.15 | pKi | 7000 | nM | Ki | J Med Chem (2022) 65: 1933-1945 [PMID:34898192] |
| 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] |
| ChEMBL | Inhibition of human uPA | B | 5.62 | pIC50 | 2400 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126753-126753 [PMID:31679971] |
| ChEMBL | Inhibition of human kidney uPA using chromogenic H-D-Ile-L-propyl-L-arginine-p-nitroaniline as substrate | B | 5.62 | pIC50 | 2400 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126753-126753 [PMID:31679971] |
| 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] |
| ChEMBL | Inhibition of mouse uPA | B | 5.64 | pIC50 | 2300 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126753-126753 [PMID:31679971] |
| protein C, inactivator of coagulation factors Va and VIIIa/Vitamin K-dependent protein C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4444] [GtoPdb: 2396] [UniProtKB: P04070] | ||||||||
| ChEMBL | Inhibition of activated protein C (unknown origin) using chromogenic L-pyroGlu-L-Pro-L-Arg-p-nitroaniline as substrate | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126753-126753 [PMID:31679971] |
| 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 | J Biol Chem (1996) 271: 10433-6 [PMID:8631835] |
| 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 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]
