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Target
11-beta-hydroxysteroid dehydrogenase 1
Ligand
BDBM32558
Substrate
BDBM13739
Meas. Tech.
Human 11beta-HSD1 SPA Assay
IC50
184±n/a nM
Citation
 Sun, D; Wang, Z; Di, Y; Jaen, JC; Labelle, M; Ma, J; Miao, S; Sudom, A; Tang, L; Tomooka, CS; Tu, H; Ursu, S; Walker, N; Yan, X; Ye, Q; Powers, JP Discovery and initial SAR of arylsulfonylpiperazine inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). Bioorg Med Chem Lett 18:3513-6 (2008) [PubMed]  Article 
Target
Name:
11-beta-hydroxysteroid dehydrogenase 1
Synonyms:
11-DH | 11-beta-HSD1 | 11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1) | 11-beta-hydroxysteroid dehydrogenase 1 | 11beta-HSD1A | Corticosteroid 11-beta-dehydrogenase isozyme 1 | Corticosteroid 11-beta-dehydrogenase isozyme 1 (11-beta-HSD-1) | DHI1_MOUSE | Hsd11 | Hsd11b1
Type:
Enzyme
Mol. Mass.:
32369.70
Organism:
Mus musculus (mouse)
Description:
P50172
Residue:
292
Sequence:
MAVMKNYLLPILVLFLAYYYYSTNEEFRPEMLQGKKVIVTGASKGIGREMAYHLSKMGAHVVLTARSEEGLQKVVSRCLELGAASAHYIAGTMEDMTFAEQFIVKAGKLMGGLDMLILNHITQTSLSLFHDDIHSVRRVMEVNFLSYVVMSTAALPMLKQSNGSIAVISSLAGKMTQPMIAPYSASKFALDGFFSTIRTELYITKVNVSITLCVLGLIDTETAMKEISGIINAQASPKEECALEIIKGTALRKSEVYYDKSPLTPILLGNPGRKIMEFFSLRYYNKDMFVSN
  
Inhibitor
Name:
BDBM32558
Synonyms:
arylsulfonylpiperazine, 30
Type:
Small organic molecule
Emp. Form.:
C20H25ClN2O2S
Mol. Mass.:
392.943
SMILES:
CC(C)(C)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccccc1Cl
Structure:
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Substrate
Name:
BDBM13739
Synonyms:
(1S,2R,10S,11S,14R,15S)-14-hydroxy-14-(2-hydroxyacetyl)-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-ene-5,17-dione | [3H]-cortisone | [3H]cortisone | cortisone
Type:
Steroid
Emp. Form.:
C21H28O5
Mol. Mass.:
360.444
SMILES:
[H][C@@]12CC[C@](O)(C(=O)CO)[C@@]1(C)CC(=O)[C@@]1([H])[C@@]2([H])CCC2=CC(=O)CC[C@]12C |t:23|
Structure:
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