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Target11-beta-hydroxysteroid dehydrogenase 1
LigandBDBM22472
Substrate/CompetitorBDBM13739
Meas. Tech.Human 11beta-HSD1 Scintillation Proximity Assay (SPA)
pH7.2±n/a
Temperature295.15±n/a K
Ki 13±9 nM
Citation Johansson LFotsch CBartberger MDCastro VMChen MEmery MGustafsson SHale CHickman DHoman EJordan SRKomorowski RLi AMcRae KMoniz GMatsumoto GOrihuela CPalm GVeniant MWang MWilliams MZhang J 2-Amino-1,3-thiazol-4(5H)-ones as Potent and Selective 11beta-Hydroxysteroid Dehydrogenase Type 1 Inhibitors: Enzyme-Ligand Co-Crystal Structure and Demonstration of Pharmacodynamic Effects in C57Bl/6 Mice. J Med Chem 51:2933-43 (2008) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   Solution Info,  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 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)
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:
BDBM22472
BDBM13739
NameBDBM22472
Synonyms:2-Amino-1,3-thiazol-4(5H)-one, 7b | 5,5-diethyl-2-{tricyclo[3.3.1.0^{3,7}]nonan-3-ylamino}-4,5-dihydro-1,3-thiazol-4-one
TypeSmall organic molecule
Emp. Form.C16H24N2OS
Mol. Mass.292.44
SMILESCCC1(CC)SC(NC23CC4CC2CC(C3)C4)=NC1=O |c:19,TLB:15:14:8.9:11,7:8:11:14.13.16,7:8:13:10.11.16,THB:9:8:13:10.11.16,9:10:8.15:13,15:8:11:14.13.16|
Structure
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