Reaction Details |
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Target | Polyunsaturated fatty acid 5-lipoxygenase |
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Ligand | BDBM50591532 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2200644 (CHEMBL5113160) |
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IC50 | 280±n/a nM |
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Citation | Cerqua, I; Musella, S; Peltner, LK; D'Avino, D; Di Sarno, V; Granato, E; Vestuto, V; Di Matteo, R; Pace, S; Ciaglia, T; Bilancia, R; Smaldone, G; Di Matteo, F; Di Micco, S; Bifulco, G; Pepe, G; Basilicata, MG; Rodriquez, M; Gomez-Monterrey, IM; Campiglia, P; Ostacolo, C; Roviezzo, F; Werz, O; Rossi, A; Bertamino, A Discovery and Optimization of Indoline-Based Compounds as Dual 5-LOX/sEH Inhibitors: J Med Chem65:14456-14480 (2022) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Polyunsaturated fatty acid 5-lipoxygenase |
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Name: | Polyunsaturated fatty acid 5-lipoxygenase |
Synonyms: | 5-LO | 5-Lipo-oxygenase (5-LOX) | 5-Lipoxygenase (5-LO) | 5-Lipoxygenase (LOX) | 5-Lipoygenase | 5-lipoxygenase/FLAP | ALOX5 | Arachidonate 5-lipoxygenase | LOG5 | LOX5_HUMAN |
Type: | Enzyme |
Mol. Mass.: | 77972.74 |
Organism: | Homo sapiens (Human) |
Description: | Recombinant protein was purified from E. coli lysate. After ammonium sulfate precipitation and subsequent steps, the supernatant (S100) was used for 5-LO activity assay.
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Residue: | 674 |
Sequence: | MPSYTVTVATGSQWFAGTDDYIYLSLVGSAGCSEKHLLDKPFYNDFERGAVDSYDVTVDE
ELGEIQLVRIEKRKYWLNDDWYLKYITLKTPHGDYIEFPCYRWITGDVEVVLRDGRAKLA
RDDQIHILKQHRRKELETRQKQYRWMEWNPGFPLSIDAKCHKDLPRDIQFDSEKGVDFVL
NYSKAMENLFINRFMHMFQSSWNDFADFEKIFVKISNTISERVMNHWQEDLMFGYQFLNG
CNPVLIRRCTELPEKLPVTTEMVECSLERQLSLEQEVQQGNIFIVDFELLDGIDANKTDP
CTLQFLAAPICLLYKNLANKIVPIAIQLNQIPGDENPIFLPSDAKYDWLLAKIWVRSSDF
HVHQTITHLLRTHLVSEVFGIAMYRQLPAVHPIFKLLVAHVRFTIAINTKAREQLICECG
LFDKANATGGGGHVQMVQRAMKDLTYASLCFPEAIKARGMESKEDIPYYFYRDDGLLVWE
AIRTFTAEVVDIYYEGDQVVEEDPELQDFVNDVYVYGMRGRKSSGFPKSVKSREQLSEYL
TVVIFTASAQHAAVNFGQYDWCSWIPNAPPTMRAPPPTAKGVVTIEQIVDTLPDRGRSCW
HLGAVWALSQFQENELFLGMYPEEHFIEKPVKEAMARFRKNLEAIVSVIAERNKKKQLPY
YYLSPDRIPNSVAI
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BDBM50591532 |
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n/a |
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Name | BDBM50591532 |
Synonyms: | CHEMBL4590950 |
Type | Small organic molecule |
Emp. Form. | C22H26FN3O |
Mol. Mass. | 367.4597 |
SMILES | Fc1ccc(CN2CCc3cc(NC(=O)NC4CCCCC4)ccc23)cc1 |
Structure |
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