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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 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]