OL135 [Ligand Id: 5235] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL177577 (OL-135)
  • carboxylesterase 1/Acyl coenzyme A:cholesterol acyltransferase in Human [ChEMBL: CHEMBL2265] [GtoPdb: 2592] [UniProtKB: P23141]
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  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Human [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519]
  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Mouse [ChEMBL: CHEMBL3455] [GtoPdb: 1400] [UniProtKB: O08914]
  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612]
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  • Fatty acid amide hydrolase-2/Fatty-acid amide hydrolase 2 in Human [ChEMBL: CHEMBL1628475] [GtoPdb: 1401] [UniProtKB: Q6GMR7]
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  • Neutral cholesterol ester hydrolase 1 in Human [ChEMBL: CHEMBL5048] [UniProtKB: Q6PIU2]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]