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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 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]