CAY10499 [Ligand Id: 12994] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL570812
  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Human [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519]
  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612]
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  • monoacylglycerol lipase/Monoglyceride lipase in Human [ChEMBL: CHEMBL4191] [GtoPdb: 1399] [UniProtKB: Q99685]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Fatty acid amide hydrolase/Anandamide amidohydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519]
ChEMBL Inhibition of human recombinant FAAH-maltose binding protein B 7.11 pIC50 77.62 nM IC50 J Med Chem (2009) 52: 7310-7314 [PMID:19883085]
ChEMBL Inhibition of FAAH (unknown origin) B 7.12 pIC50 76 nM IC50 Eur J Med Chem (2013) 63: 64-75 [PMID:23455058]
GtoPdb - - 7.85 pIC50 14 nM IC50 J Enzyme Inhib Med Chem (2016) 31: 137-46 [PMID:25669350]
ChEMBL Inhibition of human recombinant FAAH using AMC arachidonoyl amide as substrate after 30 mins by fluorescence assay B 7.85 pIC50 14 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 7.89 pIC50 13 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 30 mins followed by substrate addition by fluorescence assay B 8.46 pIC50 3.5 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 60 mins followed by substrate addition by fluorescence assay B 8.72 pIC50 1.9 nM IC50 Eur J Med Chem (2015) 97: 289-305 [PMID:26002335]
Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612]
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 5.89 pIC50 1300 nM IC50 Eur J Med Chem (2013) 63: 64-75 [PMID:23455058]
ChEMBL Inhibition of rat FAAH B 7.07 pIC50 86 nM IC50 J Med Chem (2017) 60: 4-46 [PMID:27766867]
ChEMBL Inhibition of rat FAAH B 7.07 pIC50 86 nM IC50 J Med Chem (2020) 63: 5783-5796 [PMID:32429662]
monoacylglycerol lipase/Monoglyceride lipase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4191] [GtoPdb: 1399] [UniProtKB: Q99685]
ChEMBL Inhibition of human recombinant MAGL-mediated 1,3-dihydroxypropan-1-yl 4-pyren-1-ylbutanoate conversion to 4-pyren-1-ylbutanoic acid preincubated for 15 mins measured after 45 mins by HPLC analysis B 6.32 pIC50 480 nM IC50 Eur J Med Chem (2013) 63: 64-75 [PMID:23455058]
ChEMBL Inhibition of recombinant human MAGL using 1,3-dihydroxypropan-2-yl 4-pyren-1-yl-butanoate as substrate after 45 mins by fluorescence-based reversed phase HPLC analysis B 6.32 pIC50 480 nM IC50 Bioorg Med Chem (2017) 25: 825-837 [PMID:27989417]
ChEMBL Inhibition of human recombinant MAGL using 1,3-dihydroxypropan-2-yl 4-pyren-1-ylbutanoate as substrate measured after 45 mins by reverse-phase HPLC-based fluorescence assay B 6.32 pIC50 480 nM IC50 J Med Chem (2020) 63: 13159-13186 [PMID:33089691]
ChEMBL Inhibition of human MAGL using 4-Nitrophenylacetate as substrate B 6.37 pIC50 424 nM IC50 Eur J Med Chem (2016) 121: 318-330 [PMID:27267002]
ChEMBL Inhibition of MAGL (unknown origin) using 4-nitrophenylacetate as substrate B 6.4 pIC50 400 nM IC50 Eur J Med Chem (2013) 63: 64-75 [PMID:23455058]
ChEMBL Inhibition of human recombinant MAGL using 4-nitrophenylacetate as substrate B 6.84 pIC50 146 nM IC50 Bioorg Med Chem (2014) 22: 3285-3291 [PMID:24853323]
GtoPdb - - 6.84 pIC50 144 nM IC50 J Enzyme Inhib Med Chem (2016) 31: 137-46 [PMID:25669350]
ChEMBL Inhibition of human recombinant MAGL using 4-nitrophenylacetate as substrate after 30 mins B 6.84 pIC50 144 nM IC50 Bioorg Med Chem (2014) 22: 3285-3291 [PMID:24853323]
ChEMBL Inhibition of recombinant human C-terminal His-tagged MAGL expressed in Escherichia coli using 4-NPA as substrate measured after 30 mins B 6.85 pIC50 140 nM IC50 Eur J Med Chem (2018) 157: 817-836 [PMID:30144699]
ChEMBL Inhibition of recombinant human MAGL using 4-NPA as substrate after 30 mins by colorimetric analysis B 6.85 pIC50 140 nM IC50 J Med Chem (2018) 61: 1340-1354 [PMID:29309142]
ChEMBL Inhibition of human recombinant MAGL using 4-NPA substrate incubated for 30 mins B 6.87 pIC50 134 nM IC50 J Med Chem (2016) 59: 10299-10314 [PMID:27809504]
ChEMBL Inhibition of human recombinant MAGL using 4-NPA as substrate after 30 mins B 6.87 pIC50 134 nM IC50 J Med Chem (2019) 62: 1932-1958 [PMID:30715876]
ChEMBL Inhibition of human recombinant MAGL using 4-nitrophenylacetate as substrate incubated for 30 mins by microplate reader assay B 6.89 pIC50 130 nM IC50 Eur J Med Chem (2021) 209: 112857-112857 [PMID:33045662]
ChEMBL Inhibition of recombinant human MAGL B 7.04 pIC50 92 nM IC50 J Med Chem (2017) 60: 4-46 [PMID:27766867]
ChEMBL Inhibition of MAGL (unknown origin) B 7.04 pIC50 92 nM IC50 Eur J Med Chem (2013) 63: 64-75 [PMID:23455058]
ChEMBL Inhibition of human recombinant MAGL B 7.04 pIC50 92 nM IC50 J Med Chem (2020) 63: 5783-5796 [PMID:32429662]
ChEMBL Inhibition of human recombinant MAGL using 4-nitrophenylacetate as substrate preincubated for 30 mins followed by substrate addition B 7.59 pIC50 26 nM IC50 Bioorg Med Chem (2014) 22: 3285-3291 [PMID:24853323]
ChEMBL Inhibition of human MGL activity using [3H]2-oleoylglycerol substrate by liquid scintillation counting B 7.69 pIC50 20.42 nM IC50 J Med Chem (2009) 52: 7310-7314 [PMID:19883085]
ChEMBL Inhibition of MAGL (unknown origin) B 7.7 pIC50 20 nM IC50 Eur J Med Chem (2016) 121: 318-330 [PMID:27267002]
ChEMBL Inhibition of human MAGL using 4-Nitrophenylacetate substrate incubated for 15 mins B 7.7 pIC50 20 nM IC50 Bioorg Med Chem Lett (2014) 24: 3986-3996 [PMID:25011912]
ChEMBL Inhibition of MAGL (unknown origin) B 7.7 pIC50 20 nM IC50 Bioorg Med Chem Lett (2021) 41: 127986-127986 [PMID:33766770]
ChEMBL Inhibition of human recombinant MAGL using 4-nitrophenylacetate as substrate preincubated for 60 mins followed by substrate addition B 8.05 pIC50 9 nM IC50 Bioorg Med Chem (2014) 22: 3285-3291 [PMID:24853323]

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]