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Target
11-beta-hydroxysteroid dehydrogenase type 2
Ligand
BDBM29830
Substrate
BDBM13775
Meas. Tech.
11beta-HSD2 Homogeneous Time-Resolved Fluorescence (HTRF) Assay
pH
7.8000±n/a
Temperature
295.1500±n/a K
IC50
>100000±n/a nM
Citation
 Lepifre, F; Christmann-Franck, S; Roche, D; Leriche, C; Carniato, D; Charon, C; Bozec, S; Doare, L; Schmidlin, F; Lecomte, M; Valeur, E Discovery and structure-guided drug design of inhibitors of 11beta-hydroxysteroid-dehydrogenase type I based on a spiro-carboxamide scaffold. Bioorg Med Chem Lett 19:3682-5 (2009) [PubMed]  Article 
Target
Name:
11-beta-hydroxysteroid dehydrogenase type 2
Synonyms:
11-beta-hydroxysteroid dehydrogenase type 2 | NAD-dependent 11-beta-hydroxysteroid dehydrogenase | 11-DH2 | 11-beta-HSD2 | 11-beta-hydroxysteroid dehydrogenase type 2 (11-beta-HSD2) | 11-beta-Hydroxysteroid Dehydrogenase 2 (11-beta-HSD2) | Corticosteroid 11-beta-dehydrogenase isozyme 2 | DHI2_HUMAN | HSD11B2 | HSD11K | SDR9C3 | 11-beta-hydroxysteroid dehydrogenase | 11-beta-hydroxysteroid dehydrogenase 2
Type:
Enzyme
Mol. Mass.:
44141.72
Organism:
Human
Description:
Purified recombinant human 11beta-HSD2.
Residue:
405
Sequence:
MERWPWPSGGAWLLVAARALLQLLRSDLRLGRPLLAALALLAALDWLCQRLLPPPAALAVLAAAGWIALSRLARPQRLPVATRAVLITGCDSGFGKETAKKLDSMGFTVLATVLELNSPGAIELRTCCSPRLRLLQMDLTKPGDISRVLEFTKAHTTSTGLWGLVNNAGHNEVVADAELSPVATFRSCMEVNFFGALELTKGLLPLLRSSRGRIVTVGSPAGDMPYPCLGAYGTSKAAVALLMDTFSCELLPWGVKVSIIQPGCFKTESVRNVGQWEKRKQLLLANLPQELLQAYGKDYIEHLHGQFLHSLRLAMSDLTPVVDAITDALLAARPRRRYYPGQGLGLMYFIHYYLPEGLRRRFLQAFFISHCLPRALQPGQPGTTPPQDAAQDPNLSPGPSPAVAR
  
Inhibitor
Name:
BDBM29830
Synonyms:
spiro-carboxamide scaffold, 3
Type:
Small organic molecule
Emp. Form.:
TBD
Mol. Mass.:
TBD
SMILES:
TBD
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM13775
Synonyms:
[3H]cortisol | (1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-hydroxyacetyl)-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-en-5-one | cortisol | 3H-cortisol | 11beta,17alpha,21-Trihydroxy-4-pregnene-3,20-dione | HYDROCORTISONE | US10188667, Example 00023
Type:
Steroid
Emp. Form.:
TBD
Mol. Mass.:
TBD
SMILES:
TBD
Structure:
Search PDB for entries with ligand similarity: