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ChEMBL ligand: CHEMBL570812 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]