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Target11-beta-hydroxysteroid dehydrogenase 1
LigandBDBM107487
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1685710 (CHEMBL4036189)
IC50 0.800000±n/a nM
Citation Zhuang, LTice, CMXu, ZZhao, WCacatian, SYe, YJSingh, SBLindblom, PMcKeever, BMKrosky, PMZhao, YLala, DKruk, BAMeng, SHoward, LJohnson, JABukhtiyarov, YPanemangalore, RGuo, JGuo, RHimmelsbach, FHamilton, BSchuler-Metz, ASchauerte, HGregg, RMcGeehan, GMLeftheris, KClaremon, DA Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11? hydroxysteroid dehydrogenase type 1 inhibitor. Bioorg Med Chem25:3649-3657 (2017) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
11-beta-hydroxysteroid dehydrogenase 1
Name:11-beta-hydroxysteroid dehydrogenase 1
Synonyms:11-DH | 11-beta-HSD1 | 11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1) | 11-beta-hydroxysteroid dehydrogenase | 11-beta-hydroxysteroid dehydrogenase 1 (11HSD1) | Corticosteroid 11-beta-dehydrogenase isozyme 1 | Corticosteroid 11-beta-dehydrogenase isozyme 1 (11-beta-HSD-1) | Corticosteroid 11-beta-dehydrogenase isozyme 1 (11-beta-HSD1) | Corticosteroid 11-beta-dehydrogenase isozyme 1 (11beta-HSD1) | DHI1_HUMAN | HSD11 | HSD11B1 | HSD11L | SDR26C1
Type:Enzyme
Mol. Mass.:32409.16
Organism:Homo sapiens (Human)
Description:P28845
Residue:292
Sequence:
MAFMKKYLLPILGLFMAYYYYSANEEFRPEMLQGKKVIVTGASKGIGREMAYHLAKMGAH
VVVTARSKETLQKVVSHCLELGAASAHYIAGTMEDMTFAEQFVAQAGKLMGGLDMLILNH
ITNTSLNLFHDDIHHVRKSMEVNFLSYVVLTVAALPMLKQSNGSIVVVSSLAGKVAYPMV
AAYSASKFALDGFFSSIRKEYSVSRVNVSITLCVLGLIDTETAMKAVSGIVHMQAAPKEE
CALEIIKGGALRQEEVYYDSSLWTTLLIRNPCRKILEFLYSTSYNMDRFINK
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  Blast E-value cutoff:
BDBM107487
n/a
NameBDBM107487
Synonyms:US8575157, 201 | US8592410, Comparator 13 | US8598163, 71
TypeSmall organic molecule
Emp. Form.C22H25BrFNO3
Mol. Mass.450.341
SMILESC[C@H](N1CC[C@@](CC(C)(C)O)(OC1=O)c1ccc(F)cc1)c1ccc(Br)cc1 |r|
Structure
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