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ChEMBL ligand: CHEMBL177577 (OL-135) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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carboxylesterase 1/Acyl coenzyme A:cholesterol acyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2265] [GtoPdb: 2592] [UniProtKB: P23141] | ||||||||
ChEMBL | Inhibitory concentration against Triacylglycerol hydrolase | B | 6.22 | pIC50 | 600 | nM | IC50 | J Med Chem (2005) 48: 1849-1856 [PMID:15771430] |
ChEMBL | Inhibitory concentration of triacylgylcerol hydrolase using FP-Rh radioligand | B | 6.22 | pIC50 | 600 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1423-1428 [PMID:15713400] |
ChEMBL | Inhibition of TGH | B | 6.22 | pIC50 | 600 | nM | IC50 | J Med Chem (2007) 50: 1058-1068 [PMID:17279740] |
ChEMBL | Inhibition of TGH | B | 6.22 | pIC50 | >600 | nM | IC50 | J Med Chem (2008) 51: 937-947 [PMID:18247553] |
ChEMBL | Inhibition of TGH | B | 6.22 | pIC50 | 600 | nM | IC50 | J Med Chem (2008) 51: 4392-4403 [PMID:18630870] |
ChEMBL | Inhibition of TGH | B | 6.22 | pIC50 | 600 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5842-5846 [PMID:18639454] |
Fatty acid amide hydrolase/Anandamide amidohydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519] | ||||||||
ChEMBL | Inhibition of FAAH | B | 5.33 | pKi | 4700 | nM | Ki | J Med Chem (2008) 51: 7327-7343 [PMID:18983142] |
ChEMBL | Inhibition of human recombinant FAAH | B | 8.05 | pKi | 9 | nM | Ki | Bioorg Med Chem (2008) 16: 1562-1595 [PMID:18053726] |
ChEMBL | Inhibitory constant determined against recombinant Fatty-acid amide hydrolase from human expressed in COS-7 cells | B | 8.05 | pKi | 9 | nM | Ki | J Med Chem (2005) 48: 1849-1856 [PMID:15771430] |
ChEMBL | Inhibition of human recombinant FAAH expressed in african green monkey COS7 cells | B | 8.05 | pKi | 9 | nM | Ki | J Med Chem (2008) 51: 4392-4403 [PMID:18630870] |
ChEMBL | Inhibition of rat recombinant FAAH expressed in Escherichia coli by [14C]oleamide breakdown | B | 8.33 | pKi | 4.7 | nM | Ki | J Med Chem (2007) 50: 1058-1068 [PMID:17279740] |
ChEMBL | Inhibition of FAAH | B | 8.33 | pKi | 4.7 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4674-4685 [PMID:21764305] |
ChEMBL | Inhibition of FAAH at pH 9 | B | 8.33 | pKi | 4.7 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 5847-5850 [PMID:18644727] |
ChEMBL | Inhibition of FAAH | B | 8.33 | pKi | 4.7 | nM | Ki | J Med Chem (2008) 51: 937-947 [PMID:18247553] |
ChEMBL | Inhibition of human recombinant FAAH | B | 6.2 | pIC50 | 628 | nM | IC50 | J Med Chem (2012) 55: 6898-6915 [PMID:22779702] |
ChEMBL | Inhibition of FAAH | B | 6.64 | pIC50 | 230 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4241-4244 [PMID:19515560] |
ChEMBL | Inhibition of human FAAH incubated 1 hr prior to addition of arachidonyl-amino-methyl-coumarin amide | B | 6.92 | pIC50 | 119 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4241-4244 [PMID:19515560] |
GtoPdb | - | - | 7.4 | pIC50 | 39.8 | nM | IC50 | J Biol Chem (2006) 281: 36569-78 [PMID:17015445] |
ChEMBL | Reversible inhibition of human recombinant FAAH using N-arachidonyl-7-amino-4-methylcoumarin as substrate preincubated for 20 mins before substrate addition by fluorescence assay | B | 7.48 | pIC50 | 33 | nM | IC50 | Bioorg Med Chem (2013) 21: 5188-5197 [PMID:23891163] |
ChEMBL | Inhibition of human FAAH | B | 7.82 | pIC50 | 15 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 2109-2113 [PMID:18289847] |
ChEMBL | Inhibitory concentration of fatty acid amide hydrolase using FP-Rh radioligand | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1423-1428 [PMID:15713400] |
ChEMBL | Inhibition of human transmembrane domain deficient FFAH expressed in Escherichia coli using AAMCA as substrate incubated for 1 min measured for 50 mins by fluorescence assay | B | 8.28 | pIC50 | 5.2 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 238-243 [PMID:30503633] |
ChEMBL | Reversible inhibition of human recombinant FAAH assessed as hydrolysis of [3H]-AEA after 10 mins by liquid scintillation counting | B | 8.33 | pIC50 | 4.7 | nM | IC50 | J Med Chem (2011) 54: 6812-6823 [PMID:21899370] |
ChEMBL | Inhibition of rat recombinant FAAH expressed in Escherichia coli by [14C]oleamide breakdown | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2007) 50: 1058-1068 [PMID:17279740] |
ChEMBL | Inhibitory concentration against Fatty-acid amide hydrolase | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2005) 48: 1849-1856 [PMID:15771430] |
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 | 9.4 | pIC50 | 0.4 | 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 | Inhibitor affinity towards enzymes of class serine hydrolase was determined using biotin or fluorescent as radioligand (FP-biotin or FP-Rh) | B | 8.33 | pKi | 4.7 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1423-1428 [PMID:15713400] |
ChEMBL | Inhibition of mouse FAAH | B | 8.33 | pKi | 4.7 | nM | Ki | Bioorg Med Chem (2014) 22: 2763-2770 [PMID:24690529] |
Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612] | ||||||||
ChEMBL | Inhibition of rat recombinant FAAH expressed in Escherichia coli using [14C]oleamide as substrate assessed as oleic acid formation by Dixon plot analysis | B | 8.33 | pKi | 4.7 | nM | Ki | Bioorg Med Chem (2014) 22: 2763-2770 [PMID:24690529] |
ChEMBL | Binding affinity against purified rat Fatty-acid amide hydrolase (FAAH) expressed in Escherichia coli | B | 8.33 | pKi | 4.7 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 103-106 [PMID:15582420] |
ChEMBL | Inhibition of rat recombinant FAAH expressed in Escherichia coli | B | 8.33 | pKi | 4.7 | nM | Ki | J Med Chem (2007) 50: 3359-3368 [PMID:17559203] |
ChEMBL | Inhibition of rat FAAH | B | 8.33 | pKi | 4.7 | nM | Ki | Bioorg Med Chem (2008) 16: 1562-1595 [PMID:18053726] |
ChEMBL | Inhibition of rat FAAH preincubated for 20 mins | B | 8.33 | pKi | 4.7 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 4838-4843 [PMID:18693015] |
ChEMBL | Inhibition of rat cortex FAAH by [3H]anandamide carbon filtration assay | B | 8.33 | pKi | 4.7 | nM | Ki | J Med Chem (2009) 52: 170-180 [PMID:19072118] |
ChEMBL | Inhibition of rat FAAH expressed in Escherichia coli | B | 8.33 | pKi | 4.7 | nM | Ki | J Med Chem (2008) 51: 4392-4403 [PMID:18630870] |
ChEMBL | Inhibition of rat FAAH expressed in Escherichia coli at pH 9.0 | B | 8.33 | pKi | 4.7 | nM | Ki | J Med Chem (2008) 51: 4392-4403 [PMID:18630870] |
ChEMBL | Inhibition of rat FAAH | B | 8.33 | pKi | 4.7 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 5842-5846 [PMID:18639454] |
ChEMBL | Inhibition of rat recombinant FAAH expressed in Escherichia coli | B | 8.33 | pKi | 4.7 | nM | Ki | J Med Chem (2010) 53: 230-240 [PMID:19924997] |
ChEMBL | Inhibition of rat recombinant FAAH expressed in Escherichia coli | B | 8.33 | pKi | 4.7 | nM | Ki | Bioorg Med Chem (2012) 20: 1100-1112 [PMID:22196515] |
ChEMBL | Inhibitory constant determined against recombinant Fatty-acid amide hydrolase from rat expressed in Escherichia coli | B | 8.33 | pKi | 4.7 | nM | Ki | J Med Chem (2005) 48: 1849-1856 [PMID:15771430] |
ChEMBL | Time-dependent inhibition of recombinant rat FAAH expressed in Escherichia coli assessed as breakdown of [14C]-oleamide preincubated for 1 hr by Dixon plot analysis | B | 8.38 | pKi | 4.2 | nM | Ki | J Med Chem (2014) 57: 1079-1089 [PMID:24456116] |
ChEMBL | Time-dependent inhibition of recombinant rat FAAH expressed in Escherichia coli assessed as breakdown of [14C]-oleamide preincubated for 3 hrs by Dixon plot analysis | B | 8.42 | pKi | 3.8 | nM | Ki | J Med Chem (2014) 57: 1079-1089 [PMID:24456116] |
ChEMBL | Time-dependent inhibition of recombinant rat FAAH expressed in Escherichia coli assessed as breakdown of [14C]-oleamide preincubated for 6 hrs by Dixon plot analysis | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (2014) 57: 1079-1089 [PMID:24456116] |
ChEMBL | Inhibition of rat FAAH incubated 3 hrs prior to addition of arachidonyl-amino-methyl-coumarin amide | B | 6.51 | pIC50 | 306 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4241-4244 [PMID:19515560] |
ChEMBL | Inhibition of rat FAAH incubated 1 hr prior to addition of arachidonyl-amino-methyl-coumarin amide | B | 6.95 | pIC50 | 112 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4241-4244 [PMID:19515560] |
ChEMBL | Inhibition of rat recombinant FAAH expressed in Escherichia coli | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2008) 51: 937-947 [PMID:18247553] |
ChEMBL | Inhibition of rat FAAH | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5842-5846 [PMID:18639454] |
Fatty acid amide hydrolase-2/Fatty-acid amide hydrolase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1628475] [GtoPdb: 1401] [UniProtKB: Q6GMR7] | ||||||||
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 | 7.87 | pIC50 | 13.4 | nM | IC50 | J Med Chem (2017) 60: 4-46 [PMID:27766867] |
GtoPdb | - | - | 8.4 | pIC50 | 4 | nM | IC50 |
J Biol Chem (2006) 281: 36569-78 [PMID:17015445]; Anesth Analg (2009) 108: 316-29 [PMID:19095868] |
Neutral cholesterol ester hydrolase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5048] [UniProtKB: Q6PIU2] | ||||||||
ChEMBL | Inhibition of KIAA1363 | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2007) 50: 1058-1068 [PMID:17279740] |
ChEMBL | Inhibition of KIAA1363 | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2008) 51: 937-947 [PMID:18247553] |
ChEMBL | Inhibition of KIAA1363 hydrolase | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2008) 51: 4392-4403 [PMID:18630870] |
ChEMBL | Inhibition of KIAA1363 | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5842-5846 [PMID:18639454] |
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]