Target
17-beta-hydroxysteroid dehydrogenase type 2
Ligand
BDBM50239401
Substrate
n/a
Meas. Tech.
ChEMBL_514766 (CHEMBL977265)
IC50
>3300±n/a nM
Citation
 Fotsch, CWang, M Blockade of glucocorticoid excess at the tissue level: inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 as a therapy for type 2 diabetes. J Med Chem 51:4851-7 (2008) [PubMed]  Article 
Target
Name:
17-beta-hydroxysteroid dehydrogenase type 2
Synonyms:
17-beta-Hydroxysteroid Dehydrogenase 2 (17-beta-HSD2) | 20 alpha-hydroxysteroid dehydrogenase | 20-alpha-HSD | DHB2_HUMAN | EDH17B2 | Estradiol 17-beta-dehydrogenase 2 | Estradiol 17-beta-dehydrogenase 2 (17beta-HSD2) | HSD17B2 | Microsomal 17-beta-hydroxysteroid dehydrogenas | SDR9C2 | Testosterone 17-beta-dehydrogenase
Type:
Oxidoreductase; single-pass type II membrane protein
Mol. Mass.:
42795.29
Organism:
Homo sapiens (Human)
Description:
Enzyme was partially purified from human placenta.
Residue:
387
Sequence:
MSTFFSDTAWICLAVPTVLCGTVFCKYKKSSGQLWSWMVCLAGLCAVCLLILSPFWGLILFSVSCFLMYTYLSGQELLPVDQKAVLVTGGDCGLGHALCKYLDELGFTVFAGVLNENGPGAEELRRTCSPRLSVLQMDITKPVQIKDAYSKVAAMLQDRGLWAVINNAGVLGFPTDGELLLMTDYKQCMAVNFFGTVEVTKTFLPLLRKSKGRLVNVSSMGGGAPMERLASYGSSKAAVTMFSSVMRLELSKWGIKVASIQPGGFLTNIAGTSDKWEKLEKDILDHLPAEVQEDYGQDYILAQRNFLLLINSLASKDFSPVLRDIQHAILAKSPFAYYTPGKGAYLWICLAHYLPIGIYDYFAKRHFGQDKPMPRALRMPNYKKKAT
  
Inhibitor
Name:
BDBM50239401
Synonyms:
3-Adamantan-1-yl-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[4,3-a]azepine | CHEMBL256777 | MERCK-544
Type:
Small organic molecule
Emp. Form.:
C17H25N3
Mol. Mass.:
271.4005
SMILES:
C1C2CC3CC1CC(C2)(C3)c1nnc2CCCCCn12 |TLB:4:3:0.5.6:8,0:5:1.8.2:9,0:1:5.6.4:9,THB:4:5:8:2.3.9|
Structure:
Search PDB for entries with ligand similarity: