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Target11-beta-hydroxysteroid dehydrogenase type 2
LigandBDBM22473
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:
BDBM22473
BDBM13775
NameBDBM22473
Synonyms:2-(hexahydro-2,5-methanopentalen-3a(1H)-ylamino)-1-thia-3-azaspiro[4.4]non-2-en-4-one | 2-Amino-1,3-thiazol-4(5H)-one, 8b | 2-{tricyclo[3.3.1.0^{3,7}]nonan-3-ylamino}-1-thia-3-azaspiro[4.4]non-2-en-4-one
TypeSmall organic molecule
Emp. Form.C16H22N2OS
Mol. Mass.290.424
SMILESO=C1N=C(NC23CC4CC2CC(C3)C4)SC11CCCC1 |t:2,TLB:12:11:5.6:8,4:5:8:11.10.13,4:5:10:7.8.13,THB:6:5:10:7.8.13,6:7:5.12:10,12:5:8:11.10.13|
Structure
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