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Target11-beta-hydroxysteroid dehydrogenase 1
LigandBDBM50319659
Substrate/Competitorn/a
Meas. Tech.ChEMBL_634656 (CHEMBL1118096)
Ki 58±n/a nM
Citation Véniant, MMHale, CHungate, RWGahm, KEmery, MGJona, JJoseph, SAdams, JHague, AMoniz, GZhang, JBartberger, MDLi, VSyed, RJordan, SKomorowski, RChen, MMCupples, RKim, KWSt Jean, DJJohansson, LHenriksson, MAWilliams, MVallgårda, JFotsch, CWang, M Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221). J Med Chem53:4481-7 (2010) [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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BDBM50319659
n/a
NameBDBM50319659
Synonyms:2-(bicyclo[2.2.1]heptan-2-ylamino)-5-isopropylthiazol-4(5H)-one | CHEMBL1083563
TypeSmall organic molecule
Emp. Form.C13H20N2OS
Mol. Mass.252.376
SMILESCC(C)c1sc(NC2CC3CCC2C3)nc1O
Structure
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