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Target11-beta-hydroxysteroid dehydrogenase 1
LigandBDBM50174297
Substrate/Competitorn/a
Meas. Tech.ChEMBL_326693 (CHEMBL868712)
IC50 2.6±n/a nM
Citation Gu, XDragovic, JKoo, GCKoprak, SLLeGrand, CMundt, SSShah, KSpringer, MSTan, EYThieringer, RHermanowski-Vosatka, AZokian, HJBalkovec, JMWaddell, ST Discovery of 4-heteroarylbicyclo[2.2.2]octyltriazoles as potent and selective inhibitors of 11beta-HSD1: novel therapeutic agents for the treatment of metabolic syndrome. Bioorg Med Chem Lett15:5266-9 (2005) [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:
BDBM50174297
n/a
NameBDBM50174297
Synonyms:3-(4-(3-(2,4-difluorophenyl)-1,2,4-oxadiazol-5-yl)bicyclo[2.2.2]octan-1-yl)-4-methyl-5-(2-(trifluoromethyl)phenyl)-4H-1,2,4-triazole | CHEMBL372851
TypeSmall organic molecule
Emp. Form.C26H22F5N5O
Mol. Mass.515.4778
SMILESCn1c(nnc1C12CCC(CC1)(CC2)c1nc(no1)-c1ccc(F)cc1F)-c1ccccc1C(F)(F)F
Structure
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