Reaction Details |
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Target | Monoglyceride lipase |
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Ligand | BDBM50255777 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEBML_1687487 |
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IC50 | 24±n/a nM |
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Citation | McAllister, LA; Butler, CR; Mente, S; O'Neil, SV; Fonseca, KR; Piro, JR; Cianfrogna, JA; Foley, TL; Gilbert, AM; Harris, AR; Helal, CJ; Johnson, DS; Montgomery, JI; Nason, DM; Noell, S; Pandit, J; Rogers, BN; Samad, TA; Shaffer, CL; da Silva, RG; Uccello, DP; Webb, D; Brodney, MA Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation. J Med Chem61:3008-3026 (2018) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Monoglyceride lipase |
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Name: | Monoglyceride lipase |
Synonyms: | HU-K5 | Lysophospholipase homolog | Lysophospholipase-like | MAGL | MGL | MGLL | MGLL_HUMAN |
Type: | Hydrolase |
Mol. Mass.: | 33264.56 |
Organism: | Homo sapiens (Human) |
Description: | Human recombinant MGL (Cayman Chemical, cat# 10008354). |
Residue: | 303 |
Sequence: | MPEESSPRRTPQSIPYQDLPHLVNADGQYLFCRYWKPTGTPKALIFVSHGAGEHSGRYEE
LARMLMGLDLLVFAHDHVGHGQSEGERMVVSDFHVFVRDVLQHVDSMQKDYPGLPVFLLG
HSMGGAIAILTAAERPGHFAGMVLISPLVLANPESATTFKVLAAKVLNLVLPNLSLGPID
SSVLSRNKTEVDIYNSDPLICRAGLKVCFGIQLLNAVSRVERALPKLTVPFLLLQGSADR
LCDSKGAYLLMELAKSQDKTLKIYEGAYHVLHKELPEVTNSVFHEINMWVSQRTATAGTA
SPP
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BDBM50255777 |
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n/a |
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Name | BDBM50255777 |
Synonyms: | CHEMBL4061795 |
Type | Small organic molecule |
Emp. Form. | C21H17FN4O4 |
Mol. Mass. | 408.3825 |
SMILES | [H][C@@]12CN(C[C@]1([H])[C@H]2c1ccn(n1)-c1ccc(F)cc1)C(=O)Oc1ccc(cc1)[N+]([O-])=O |r| |
Structure |
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