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 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]