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Target
11-beta-hydroxysteroid dehydrogenase 1
Ligand
BDBM107482
Substrate
n/a
Meas. Tech.
Scintillation Proximity Assay
pH
7.4±0
IC50
14.16±0.0 nM
Citation
 Claremon, D; Tice, C; Singh, S; Ye, Y; Leftheris, K; Zhuang, L Derivatives of [1,3]Oxazin-2-one useful for the treatment of metabolic diseases such as lipid disorders US Patent  US8598163 Publication Date 12/3/2013
Target
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:
MAFMKKYLLPILGLFMAYYYYSANEEFRPEMLQGKKVIVTGASKGIGREMAYHLAKMGAHVVVTARSKETLQKVVSHCLELGAASAHYIAGTMEDMTFAEQFVAQAGKLMGGLDMLILNHITNTSLNLFHDDIHHVRKSMEVNFLSYVVLTVAALPMLKQSNGSIVVVSSLAGKVAYPMVAAYSASKFALDGFFSSIRKEYSVSRVNVSITLCVLGLIDTETAMKAVSGIVHMQAAPKEECALEIIKGGALRQEEVYYDSSLWTTLLIRNPCRKILEFLYSTSYNMDRFINK
  
Inhibitor
Name:
BDBM107482
Synonyms:
US8575157, 190 | US8592410, Comparator 2 | US8598163, 60
Type:
Small organic molecule
Emp. Form.:
C23H19F3N2O3
Mol. Mass.:
428.4038
SMILES:
OCCC1(CCN(C(=O)O1)c1cccc(n1)-c1ccc(F)cc1F)c1ccccc1F
Structure:
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