| Reaction Details |
|---|
 | Report a problem with these data |
| Target | Polyunsaturated fatty acid 5-lipoxygenase |
|---|
| Ligand | BDBM24560 |
|---|
| Substrate/Competitor | n/a |
|---|
| Meas. Tech. | ChEMBL_1277577 (CHEMBL3096453) |
|---|
| IC50 | 4100±n/a nM |
|---|
| Citation |  Hanke, T; Dehm, F; Liening, S; Popella, SD; Maczewsky, J; Pillong, M; Kunze, J; Weinigel, C; Barz, D; Kaiser, A; Wurglics, M; Lämmerhofer, M; Schneider, G; Sautebin, L; Schubert-Zsilavecz, M; Werz, O Aminothiazole-featured pirinixic acid derivatives as dual 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 inhibitors with improved potency and efficiency in vivo. J Med Chem56:9031-44 (2013) [PubMed] Article |
|---|
| More Info.: | Get all data from this article, Assay Method |
|---|
| |
| Polyunsaturated fatty acid 5-lipoxygenase |
|---|
| 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.
|
|---|
| Residue: | 674 |
|---|
| Sequence: | MPSYTVTVATGSQWFAGTDDYIYLSLVGSAGCSEKHLLDKPFYNDFERGAVDSYDVTVDE
ELGEIQLVRIEKRKYWLNDDWYLKYITLKTPHGDYIEFPCYRWITGDVEVVLRDGRAKLA
RDDQIHILKQHRRKELETRQKQYRWMEWNPGFPLSIDAKCHKDLPRDIQFDSEKGVDFVL
NYSKAMENLFINRFMHMFQSSWNDFADFEKIFVKISNTISERVMNHWQEDLMFGYQFLNG
CNPVLIRRCTELPEKLPVTTEMVECSLERQLSLEQEVQQGNIFIVDFELLDGIDANKTDP
CTLQFLAAPICLLYKNLANKIVPIAIQLNQIPGDENPIFLPSDAKYDWLLAKIWVRSSDF
HVHQTITHLLRTHLVSEVFGIAMYRQLPAVHPIFKLLVAHVRFTIAINTKAREQLICECG
LFDKANATGGGGHVQMVQRAMKDLTYASLCFPEAIKARGMESKEDIPYYFYRDDGLLVWE
AIRTFTAEVVDIYYEGDQVVEEDPELQDFVNDVYVYGMRGRKSSGFPKSVKSREQLSEYL
TVVIFTASAQHAAVNFGQYDWCSWIPNAPPTMRAPPPTAKGVVTIEQIVDTLPDRGRSCW
HLGAVWALSQFQENELFLGMYPEEHFIEKPVKEAMARFRKNLEAIVSVIAERNKKKQLPY
YYLSPDRIPNSVAI
|
|
|
|---|
| BDBM24560 |
|---|
| n/a |
|---|
| Name | BDBM24560 |
|---|
| Synonyms: | 2-({4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl}sulfanyl)octanoic acid | CHEMBL518038 | Pirinixic acid-based compound, 6a |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C20H26ClN3O2S |
|---|
| Mol. Mass. | 407.957 |
|---|
| SMILES | CCCCCCC(Sc1nc(Cl)cc(Nc2cccc(C)c2C)n1)C(O)=O |
|---|
| Structure | 
|
|---|
Search and Browse
