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Target11-beta-hydroxysteroid dehydrogenase type 2
LigandBDBM22466
Substrate/CompetitorBDBM13775
Meas. Tech.Human 11beta-HSD1 Scintillation Proximity Assay (SPA)
IC50>10000±n/a 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 Chem51:2933-43 (2008) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
11-beta-hydroxysteroid dehydrogenase type 2
Name:11-beta-hydroxysteroid dehydrogenase type 2
Synonyms:11-DH2 | 11-beta-HSD2 | 11-beta-Hydroxysteroid Dehydrogenase 2 (11-beta-HSD2) | 11-beta-hydroxysteroid dehydrogenase | 11-beta-hydroxysteroid dehydrogenase 2 | 11-beta-hydroxysteroid dehydrogenase type 2 | 11-beta-hydroxysteroid dehydrogenase type 2 (11-beta-HSD2) | Corticosteroid 11-beta-dehydrogenase isozyme 2 | DHI2_HUMAN | HSD11B2 | HSD11K | NAD-dependent 11-beta-hydroxysteroid dehydrogenase | SDR9C3
Type:Enzyme
Mol. Mass.:44141.72
Organism:Homo sapiens (Human)
Description:Purified recombinant human 11beta-HSD2.
Residue:405
Sequence:
MERWPWPSGGAWLLVAARALLQLLRSDLRLGRPLLAALALLAALDWLCQRLLPPPAALAV
LAAAGWIALSRLARPQRLPVATRAVLITGCDSGFGKETAKKLDSMGFTVLATVLELNSPG
AIELRTCCSPRLRLLQMDLTKPGDISRVLEFTKAHTTSTGLWGLVNNAGHNEVVADAELS
PVATFRSCMEVNFFGALELTKGLLPLLRSSRGRIVTVGSPAGDMPYPCLGAYGTSKAAVA
LLMDTFSCELLPWGVKVSIIQPGCFKTESVRNVGQWEKRKQLLLANLPQELLQAYGKDYI
EHLHGQFLHSLRLAMSDLTPVVDAITDALLAARPRRRYYPGQGLGLMYFIHYYLPEGLRR
RFLQAFFISHCLPRALQPGQPGTTPPQDAAQDPNLSPGPSPAVAR
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  Blast E-value cutoff:
BDBM22466
BDBM13775
NameBDBM22466
Synonyms:2-Amino-1,3-thiazol-4(5H)-one, 5h | 5-ethyl-5-methyl-2-{tricyclo[3.3.1.0^{3,7}]nonan-3-ylamino}-4,5-dihydro-1,3-thiazol-4-one
TypeSmall organic molecule
Emp. Form.C15H22N2OS
Mol. Mass.278.413
SMILESCCC1(C)SC(NC23CC4CC2CC(C3)C4)=NC1=O |c:18,TLB:14:13:7.8:10,6:7:10:13.12.15,6:7:12:9.10.15,THB:8:7:12:9.10.15,8:9:7.14:12,14:7:10:13.12.15|
Structure
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