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ChEMBL ligand: CHEMBL184238 (KDS-4103, ORG-231295, Urb-597, URB 597, URB597) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Fatty acid amide hydrolase/Anandamide amidohydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519] | ||||||||
ChEMBL | Inhibition of human recombinant FAAH expressed in HEK293 cells by [3H]anandamide carbon filtration assay | B | 5.66 | pIC50 | 2187 | nM | IC50 | J Med Chem (2009) 52: 170-180 [PMID:19072118] |
ChEMBL | Inhibition of recombinant human N-terminal -His6 tagged FAAH (32 to 579 residues) expressed in Escherichia coli BL21-AI preincubated for 5 mins followed by olamide substrate addition measured every 10 sec intervals for 30 mins by spectrophotometry | B | 6.01 | pIC50 | 986 | nM | IC50 | J Med Chem (2017) 60: 4-46 [PMID:27766867] |
ChEMBL | Inhibition of human recombinant FAAH expressed in sf21 cells using AMC-AA as substrate preincubated for 15 mins followed by substrate addition measured after 2 hrs by spectrophotometric analysis | B | 6.59 | pIC50 | 260 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 2701-2705 [PMID:27117424] |
ChEMBL | Inhibition of human recombinant FAAH overexpressed in African green monkey COS7 cells using [3H]-anandamide as substrate preincubated for 10 mins before substrate addition measured after 10 mins by liquid scintillation counting analysis | B | 6.77 | pIC50 | 170 | nM | IC50 | J Med Chem (2013) 56: 8484-8496 [PMID:24083878] |
ChEMBL | Inhibition of human recombinant FAAH overexpressed in African green monkey COS7 cells using [3H]-anandamide as substrate preincubated for 10 mins before substrate addition measured after 10 mins by liquid scintillation counting analysis | B | 6.78 | pIC50 | 165.96 | nM | IC50 | J Med Chem (2013) 56: 8484-8496 [PMID:24083878] |
ChEMBL | Inhibition of FAAH | B | 6.96 | pIC50 | 109 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4241-4244 [PMID:19515560] |
ChEMBL | Inhibition of recombinant human N-terminal -His6 tagged FAAH (32 to 579 residues) expressed in Escherichia coli BL21 preincubated for 60 mins followed by olamide substrate addition measured every 10 sec intervals for 30 mins by spectrophotometry | B | 6.96 | pIC50 | 109 | nM | IC50 | J Med Chem (2017) 60: 4-46 [PMID:27766867] |
GtoPdb | - | - | 7 | pIC50 | 100 | nM | IC50 | J Biol Chem (2006) 281: 36569-78 [PMID:17015445] |
ChEMBL | Inhibition of human recombinant FAAH in assessed as hydrolysis of [14C]-anandamide preincubated for 20 mins before [14C]-anandamide addition measured after 30 mins | B | 7.05 | pIC50 | 90 | nM | IC50 | ACS Med Chem Lett (2012) 3: 182-186 [PMID:24900454] |
ChEMBL | Inhibition of human FAAH incubated 1 hr prior to addition of arachidonyl-amino-methyl-coumarin amide | B | 7.11 | pIC50 | 78 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4241-4244 [PMID:19515560] |
ChEMBL | Inhibition of human recombinant FAAH using AMC arachidonoyl amide as substrate after 30 mins by fluorescence assay | B | 7.23 | pIC50 | 59 | nM | IC50 | Eur J Med Chem (2015) 97: 289-305 [PMID:26002335] |
ChEMBL | Inhibition of human recombinant FAAH using AMC arachidonoyl amide as substrate preincubated with protein for 0 min followed by substrate addition by fluorescence assay | B | 7.24 | pIC50 | 58 | nM | IC50 | Eur J Med Chem (2015) 97: 289-305 [PMID:26002335] |
ChEMBL | Inhibition of human recombinant FAAH expressed in HEK293 cells preincubated for 5 mins before substrate addition by [3H]anandamide carbon filtration assay | B | 7.33 | pIC50 | 47 | nM | IC50 | J Med Chem (2009) 52: 170-180 [PMID:19072118] |
ChEMBL | Inhibition of human recombinant FAAH expressed in Escherichia coli using [3H]AEA substrate incubated at 37 degC for 10 mins by liquid scintillation counting method | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem (2011) 19: 3777-3786 [PMID:21612933] |
ChEMBL | Inhibition of human FAAH using N-(6-methoxypyridin-3-yl)octanamide as a substrate assessed as reduction in 6-methoxypyridin-3-amine formation by fluorescence microplate reader assay | B | 7.49 | pIC50 | 32 | nM | IC50 | Bioorg Med Chem (2021) 51: 116507-116507 [PMID:34794001] |
ChEMBL | Inhibition of human recombinant FAAH using AMC-AA as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by multimode plate reader analysis | B | 7.51 | pIC50 | 31.1 | nM | IC50 | Eur J Med Chem (2023) 246: 114952-114952 [PMID:36462439] |
ChEMBL | Inhibition of human FAAH expressed in baculovirus-infected High Five cells S9 fraction using OMP substrate by fluorescence based assay | B | 7.64 | pIC50 | 23 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 762-768 [PMID:29366648] |
ChEMBL | Inhibition of human recombinant FAAH expressed in HEK293 cells preincubated for 30 mins before substrate addition by [3H]anandamide carbon filtration assay | B | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (2009) 52: 170-180 [PMID:19072118] |
ChEMBL | Inhibition of human recombinant FAAH expressed in Escherichia coli assessed as hydrolysis of [3H]-AEA | B | 7.82 | pIC50 | 15 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 1322-1326 [PMID:24508127] |
ChEMBL | Inhibition of human recombinant FAAH using AMC arachidonoyl amide as substrate preincubated with protein for 30 mins followed by substrate addition by fluorescence assay | B | 7.89 | pIC50 | 13 | nM | IC50 | Eur J Med Chem (2015) 97: 289-305 [PMID:26002335] |
ChEMBL | Inhibition of human recombinant FAAH expressed in HEK293 cells preincubated for 60 mins before substrate addition by [3H]anandamide carbon filtration assay | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2009) 52: 170-180 [PMID:19072118] |
ChEMBL | Inhibition of human recombinant FAAH using AMC arachidonoyl amide as substrate preincubated with protein for 60 mins followed by substrate addition by fluorescence assay | B | 8.16 | pIC50 | 6.9 | nM | IC50 | Eur J Med Chem (2015) 97: 289-305 [PMID:26002335] |
ChEMBL | Inhibition of human FAAH | B | 8.34 | pIC50 | 4.6 | nM | IC50 | J Med Chem (2008) 51: 7327-7343 [PMID:18983142] |
ChEMBL | Inhibition of FAAH | B | 8.34 | pIC50 | 4.6 | nM | IC50 | J Med Chem (2012) 55: 6898-6915 [PMID:22779702] |
ChEMBL | Irreversible inhibition of human recombinant FAAH assessed as hydrolysis of [3H]-AEA after 10 mins by liquid scintillation counting | B | 8.34 | pIC50 | 4.6 | nM | IC50 | J Med Chem (2011) 54: 6812-6823 [PMID:21899370] |
ChEMBL | Inhibition of FAAH | B | 8.34 | pIC50 | 4.6 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4674-4685 [PMID:21764305] |
ChEMBL | Inhibition of human FAAH assessed as hydrolysis of anandamido-amino-methyl-cumarin | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2492-2496 [PMID:21392988] |
ChEMBL | Inhibition of FAAH (unknown origin) | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem (2013) 21: 28-41 [PMID:23218778] |
ChEMBL | Inhibition of FAAH (unknown origin) | B | 8.42 | pIC50 | 3.8 | nM | IC50 | Eur J Med Chem (2013) 63: 64-75 [PMID:23455058] |
ChEMBL | Inhibition of human FAAH expressed in HEK293-TRex cells using arachadonyl 7-amino 4-methyl coumarin amide as substrate by fluorescence assay | B | 8.52 | pIC50 | 3 | nM | IC50 | Medchemcomm (2012) 3: 1258-1263 |
ChEMBL | Inhibition of human FAAH expressed in HEK293 cells using arachadonyl 7-amino 4-methyl coumarin amide as substrate by fluorimetric assay | B | 8.64 | pIC50 | 2.3 | nM | IC50 | Medchemcomm (2012) 3: 611-619 |
ChEMBL | Inhibition of MBP-fused human recombinant FAAH with truncated N-terminal transmembrane domain expressed in Escherichia coli T7 using D-AMC substrate measured over 40 mins by fluorescence based assay | B | 9.62 | pIC50 | 0.24 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 2965-2973 [PMID:27130358] |
Fatty acid amide hydrolase/Anandamide amidohydrolase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3455] [GtoPdb: 1400] [UniProtKB: O08914] | ||||||||
ChEMBL | Inhibition of mouse FAAH isolated from brain homogenate using [3H-ethanolamine]AEA as substrate incubated for 20 mins prior to substrate addition measured after 15 mins by beta counting analysis | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2012) 55: 6898-6915 [PMID:22779702] |
ChEMBL | Inhibition of FAAH in mouse brain membranes using [14C]-AEA as substrate incubated for 15 mins by scintillation counting method | B | 6.96 | pIC50 | 110 | nM | IC50 | Eur J Med Chem (2019) 183: 111674-111674 [PMID:31518969] |
ChEMBL | Inhibition of FAAH in mouse brain microsomes using OMP substrate by fluorescence based assay | B | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 762-768 [PMID:29366648] |
ChEMBL | Inhibition of mouse FAAH isolated from brain homogenate using [3H-ethanolamine]AEA as substrate incubated for 20 mins prior to substrate addition measured after 15 mins by beta counting analysis | B | 8.34 | pIC50 | 4.6 | nM | IC50 | J Med Chem (2012) 55: 6898-6915 [PMID:22779702] |
Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612] | ||||||||
ChEMBL | Inhibition of rat cortex FAAH by [3H]anandamide carbon filtration assay | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (2009) 52: 170-180 [PMID:19072118] |
ChEMBL | Inhibition of FAAH from rat brain microsomes by RP-HPLC | B | 6.62 | pIC50 | 240 | nM | IC50 | Bioorg Med Chem (2010) 18: 945-952 [PMID:20005725] |
ChEMBL | Inhibition of FAAH in rat brain membrane at pH 7.4 using N-arachidonoyl-[14C]-ethanolamine as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by scintillation counting method | B | 6.85 | pIC50 | 140.8 | nM | IC50 | J Med Chem (2016) 59: 6387-6406 [PMID:27309570] |
ChEMBL | Inhibition of Sprague-Dawley rat brain microsome FAAH assessed as reduction in 4-pyren-1-ylbutanoic acid release after 60 mins by reverse phase HPLC-based fluorescence method | B | 7.17 | pIC50 | 67 | nM | IC50 | Bioorg Med Chem (2012) 20: 1100-1112 [PMID:22196515] |
ChEMBL | Inhibition of rat brain FAAH using [3H]AEA as substrate preincubated for 10 mins at pH 6 | B | 7.19 | pIC50 | 64 | nM | IC50 | Eur J Med Chem (2017) 136: 523-542 [PMID:28535469] |
ChEMBL | Inhibition of rat FAAH incubated 1 hr prior to addition of arachidonyl-amino-methyl-coumarin amide | B | 7.2 | pIC50 | 63 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4241-4244 [PMID:19515560] |
ChEMBL | Inhibition of FAAH in Sprague-Dawley rat brain microsomes assessed as N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide conversion to 4-pyren-1-ylbutanoic acid preincubated for 10 mins measured after 45 mins by HPLC analysis | B | 7.21 | pIC50 | 62 | nM | IC50 | Eur J Med Chem (2013) 63: 64-75 [PMID:23455058] |
ChEMBL | Inhibition of FAAH in rat brain microsomes assessed as reduction in enzyme-mediated 4-pyren-1-ylbutanoic acid release using N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide as substrate incubated fro 60 mins by reversed phase HPLC method | B | 7.22 | pIC50 | 60 | nM | IC50 | Medchemcomm (2017) 8: 616-620 [PMID:30108777] |
ChEMBL | Inhibition of FAAH in rat brain microsomes using N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide as substrate after 60 mins by fluorescence-based reversed phase HPLC analysis | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem (2017) 25: 825-837 [PMID:27989417] |
ChEMBL | Inhibition of FAAH in rat brain microsomes using N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide as substrate after 60 mins by fluorescence-based HPLC analysis | B | 7.22 | pIC50 | 60 | nM | IC50 | Eur J Med Chem (2018) 160: 183-192 [PMID:30340141] |
ChEMBL | Inhibition of Sprague-Dawley rat brain microsomal FAAH using N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide as substrate assessed as 4-pyren-1-ylbutanoic acid release preincubated for 10 mins with substrate followed by protein addition measured after 60 mins by reverse phase HPLC with fluorescence detection method | B | 7.22 | pIC50 | 60 | nM | IC50 | Medchemcomm (2014) 5: 932-936 |
ChEMBL | Inhibition of rat FAAH preincubated for 20 mins | B | 7.32 | pIC50 | 48 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 4838-4843 [PMID:18693015] |
ChEMBL | Inhibition of FAAH in rat brain membrane using N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide as substrate measured after 60 mins by reverse-phase HPLC-based fluorescence assay | B | 7.37 | pIC50 | 43 | nM | IC50 | J Med Chem (2020) 63: 13159-13186 [PMID:33089691] |
ChEMBL | Inhibition of FAAH in rat brain membrane at pH 9 using N-arachidonoyl-[14C]-ethanolamine as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins by scintillation counting method | B | 7.63 | pIC50 | 23.5 | nM | IC50 | J Med Chem (2016) 59: 6387-6406 [PMID:27309570] |
ChEMBL | Inhibition of rat FAAH incubated 3 hrs prior to addition of arachidonyl-amino-methyl-coumarin amide | B | 7.66 | pIC50 | 22 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4241-4244 [PMID:19515560] |
ChEMBL | Inhibition of rat brain FAAH using [3H]AEA as substrate preincubated for 10 mins at pH 8 | B | 7.74 | pIC50 | 18 | nM | IC50 | Eur J Med Chem (2017) 136: 523-542 [PMID:28535469] |
ChEMBL | Inhibition of FAAH in rat brain microsomes using OMP substrate by fluorescence based assay | B | 7.92 | pIC50 | 12 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 762-768 [PMID:29366648] |
ChEMBL | High Throughput FAAH Inhibition Assays: The assays for compounds described herein are amenable to high throughput screening. Preferred assays thus detect binding of the inhibitor to FAAH or the release of a reaction product (e.g., fatty acid amide or ethanolamine) produced by the hydrolysis of a substrate such as oleoylethanolamide or anandamide. The substrate may be labeled to facilitate detection of the released reaction products. High throughput assays for the presence, absence, or quantification of particular reaction products are well known to those of skill in the art. Thus, for example, U.S. Pat. No. 5,559,410 discloses high throughput screening methods for proteins, and U.S. Pat. Nos. 5,576,220 and 5,541,061 disclose high throughput methods of screening for ligand/antibody binding. | B | 8.11 | pIC50 | 7.7 | nM | IC50 | US-9187413-B2. Peripherally restricted FAAH inhibitors (2015) |
ChEMBL | Inhibition of FAAH in rat brain membranes assessed as hydrolysis of [14C]-anandamide preincubated for 20 mins before [14C]-anandamide addition measured after 30 mins | B | 8.22 | pIC50 | 6 | nM | IC50 | ACS Med Chem Lett (2012) 3: 182-186 [PMID:24900454] |
ChEMBL | Inhibition of rat histidine tagged FAAH expressed in Escherichia coli by coumarin ester substrate fluorescence assay | B | 8.31 | pIC50 | 4.9 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4585-4592 [PMID:22738638] |
ChEMBL | Inhibition of [3H]anandamide binding to fatty acid amide hydrolase of rat brain membranes | B | 8.34 | pIC50 | 4.6 | nM | IC50 | J Med Chem (2004) 47: 4998-5008 [PMID:15456244] |
ChEMBL | Inhibition of rat brain membrane FAAH | B | 8.34 | pIC50 | 4.6 | nM | IC50 | Bioorg Med Chem (2012) 20: 1100-1112 [PMID:22196515] |
ChEMBL | Inhibition of FAAH in rat brain membrane using anandamide[ethanolamine-3H] as substrate assessed as reduction in [3H]-ethanolamine production incubated for 30 mins by scintillation counting method | B | 8.34 | pIC50 | 4.6 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 2701-2705 [PMID:27117424] |
ChEMBL | Displacement of [3H]anandamide from FAAH in rat brain membranes after 30 mins by liquid scintillation counting | B | 8.34 | pIC50 | 4.6 | nM | IC50 | J Med Chem (2017) 60: 2287-2304 [PMID:28182408] |
ChEMBL | Inhibition of FAAH in rat brain membrane assessed as [3H]anandamide hydrolysis | B | 8.34 | pIC50 | 4.6 | nM | IC50 | J Med Chem (2008) 51: 3487-3498 [PMID:18507372] |
ChEMBL | Inhibition of FAAH in Wistar rat brain membranes using [3H]-anandamide as substrate preincubated for 10 mins followed by substrate addition measured after 4 mins by liquid scintillation counting method | B | 8.34 | pIC50 | 4.6 | nM | IC50 | J Med Chem (2017) 60: 4-46 [PMID:27766867] |
ChEMBL | Inhibition of FAAH1 in Wistar rat brain homogenates using [3H]anandamide as substrate incubated for 30 mins by liquid scintillation counting method | B | 8.34 | pIC50 | 4.6 | nM | IC50 | J Med Chem (2018) 61: 7902-7916 [PMID:30126274] |
ChEMBL | Inhibition of FAAH in Wistar rat brain membranes assessed as reduction in [3H]anandamide hydrolysis using [3H]anandamide as substrate preincubated for 10 mins followed by substrate addition and measured after 4 mins by HPLC/MS analysis | B | 8.34 | pIC50 | 4.6 | nM | IC50 | J Med Chem (2019) 62: 10995-11003 [PMID:31407888] |
ChEMBL | Displacement of [3H]-anandamide from rat brain FAAH after 30 mins by scintillation counting | B | 8.34 | pIC50 | 4.57 | nM | IC50 | Eur J Med Chem (2011) 46: 4466-4473 [PMID:21820769] |
ChEMBL | Inhibition of FAAH in Wistar rat cerebral membrane by liquid scintillation counting | B | 8.42 | pIC50 | 3.8 | nM | IC50 | Eur J Med Chem (2009) 44: 2994-3008 [PMID:19232787] |
ChEMBL | Inhibition of Wistar rat brain FAAH | B | 8.42 | pIC50 | 3.8 | nM | IC50 | J Med Chem (2006) 49: 4650-4656 [PMID:16854070] |
ChEMBL | Inhibition of rat FAAH assessed as hydrolysis of anandamido-amino-methyl-cumarin | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 2492-2496 [PMID:21392988] |
ChEMBL | Inhibition of rat FAAH expressed in HEK293-TRex cells using arachadonyl 7-amino 4-methyl coumarin amide as substrate by fluorescence assay | B | 8.52 | pIC50 | 3 | nM | IC50 | Medchemcomm (2012) 3: 1258-1263 |
ChEMBL | Inhibition of FAAH in Sprague-Dawley rat brain homogenates preincubated for 10 mins followed by addition of substrate measured after 30 mins by liquid scintillation counting | B | 8.77 | pIC50 | 1.7 | nM | IC50 | Eur J Med Chem (2016) 109: 216-237 [PMID:26774927] |
ChEMBL | Inhibition of rat FAAH expressed in HEK293 cells using arachadonyl 7-amino 4-methyl coumarin amide as substrate by fluorimetric assay | B | 9.15 | pIC50 | 0.7 | nM | IC50 | Medchemcomm (2012) 3: 611-619 |
ChEMBL | Inhibition of FAAH in Wistar rat brain intact neurons assessed as reduction in [3H]anandamide hydrolysis using [3H]anandamide as substrate preincubated for 10 mins followed by substrate addition and measured after 4 mins by HPLC/MS analysis | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2019) 62: 10995-11003 [PMID:31407888] |
ChEMBL | Inhibition of rat intact neuron FAAH | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Bioorg Med Chem (2012) 20: 1100-1112 [PMID:22196515] |
Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979] | ||||||||
ChEMBL | Inhibition of ovine COX1 assessed as production of PGF2-alpha preincubated with compound followed by the addition of 5 uM arachidonic acid as substrate by enzyme immunoassay | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2016) 109: 216-237 [PMID:26774927] |
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354] | ||||||||
ChEMBL | Inhibition of recombinant human COX2 assessed as production of PGF2-alpha preincubated with compound followed by the addition of 5 uM arachidonic acid as substrate by enzyme immunoassay | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2016) 109: 216-237 [PMID:26774927] |
epoxide hydrolase 2/Epoxide hydratase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2409] [GtoPdb: 2970] [UniProtKB: P34913] | ||||||||
ChEMBL | Inhibition of human recombinant soluble epoxide hydrolase expressed in baculovirus-infected High Five cells S9 fraction using CMNPC substrate by fluorescence based assay | B | 5.96 | pIC50 | 1100 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 762-768 [PMID:29366648] |
Fatty acid amide hydrolase-2/Fatty-acid amide hydrolase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1628475] [GtoPdb: 1401] [UniProtKB: Q6GMR7] | ||||||||
GtoPdb | - | - | 8.3 | pIC50 | 5.01 | nM | IC50 |
J Biol Chem (2006) 281: 36569-78 [PMID:17015445]; Anesth Analg (2009) 108: 316-29 [PMID:19095868] |
ChEMBL | Inhibition of recombinant human N-terminal FLAG-tagged/C-terminal Myc-His6 tagged FAAH2 (32 to 579 residues) expressed in COS7 cell membranes | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2017) 60: 4-46 [PMID:27766867] |
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] | ||||||||
ChEMBL | Determination of IC50 values for inhibition of enzymatic assay of human HDAC6 with custom peptide substrate | B | 6.06 | pIC50 | 873.9 | nM | IC50 | HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators |
monoacylglycerol lipase/Monoglyceride lipase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4191] [GtoPdb: 1399] [UniProtKB: Q99685] | ||||||||
ChEMBL | Inhibition of human recombinant MAGL using 7-hydroxycoumarinyl arachidonate as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by multimode plate reader analysis | B | 5.03 | pIC50 | 9384 | nM | IC50 | Eur J Med Chem (2023) 246: 114952-114952 [PMID:36462439] |
TRPA1/Transient receptor potential cation channel subfamily A member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6007] [GtoPdb: 485] [UniProtKB: O75762] | ||||||||
GtoPdb | Fluorometric Imaging Plate Reader (FLIRP) calcium-influx assay | - | 4.6 | pEC50 | 24000 | nM | EC50 | Mol Pharmacol (2007) 71: 1209-16 [PMID:17314320] |
ChEMBL | Agonist activity at human TRPA1 channel expressed in HEK293 cells assessed as increase in intracellular calcium influx | F | 4.61 | pEC50 | 24500 | nM | EC50 | J Med Chem (2010) 53: 5085-5107 [PMID:20356305] |
ChEMBL | Agonist activity at GDH-tagged human TRPA1 receptor expressed in HEK293F cells assessed as increase in intracellular Ca2+ concentration by FLIPR assay | B | 4.61 | pEC50 | 24500 | nM | EC50 | Eur J Med Chem (2013) 63: 118-132 [PMID:23474898] |
ChEMBL | Agonist activity at human TRPA1 expressed in HEK293F cells assessed as increase in calcium influx by FLIPR analysis | B | 4.61 | pEC50 | 24500 | nM | EC50 | Eur J Med Chem (2019) 170: 141-156 [PMID:30878828] |
ChEMBL | Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx by Fluo-4-AM dye based fluorescence assay | B | 7 | pEC50 | 100 | nM | EC50 | Eur J Med Chem (2019) 170: 141-156 [PMID:30878828] |
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]