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] |
| 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 (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 | US-20160067242-A1. 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 | 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 | 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 (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] |
| 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 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]
