Target
11-beta-hydroxysteroid dehydrogenase 1 [23-292,A23S,F278E]
Ligand
BDBM32499
Substrate
BDBM13739
Meas. Tech.
Scintillation Proximity Assay (SPA)
pH
6.5±n/a
Temperature
296.15±n/a K
IC50
35±n/a nM
Citation
 Wang, HRuan, ZLi, JJSimpkins, LMSmirk, RAWu, SCHutchins, RDNirschl, DSVan Kirk, KCooper, CBSutton, JCMa, ZGolla, RSeethala, RSalyan, MENayeem, AKrystek, SRSheriff, SCamac, DMMorin, PECarpenter, BRobl, JAZahler, RGordon, DAHamann, LG Pyridine amides as potent and selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1. Bioorg Med Chem Lett 18:3168-72 (2008) [PubMed]  Article 
Target
Name:
11-beta-hydroxysteroid dehydrogenase 1 [23-292,A23S,F278E]
Synonyms:
11-DH | 11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1) | Corticosteroid 11-beta-dehydrogenase isozyme 1 | DHI1_HUMAN | HSD11 | HSD11B1 | HSD11L | SDR26C1
Type:
Homodimer
Mol. Mass.:
31315.06
Organism:
Homo sapiens (Human)
Description:
P28845[23-292,A23S,F278E]
Residue:
286
Sequence:
GSHMASMTGGQQMGRGSNEEFRPEMLQGKKVIVTGASKGIGREMAYHLAKMGAHVVVTARSKETLQKVVSHCLELGAASAHYIAGTMEDMTFAEQFVAQAGKLMGGLDMLILNHITNTSLNLFHDDIHHVRKSMEVNFLSYVVLTVAALPMLKQSNGSIVVVSSLAGKVAYPMVAAYSASKFALDGFFSSIRKEYSVSRVNVSITLCVLGLIDTETAMKAVSGIVHMQAAPKEECALEIIKGGALRQEEVYYDSSRWTTLLIRNPCRKILEELYSTSYNMDRFINK
  
Inhibitor
Name:
BDBM32499
Synonyms:
pyridine amide, 8
Type:
Small organic molecule
Emp. Form.:
C19H20Cl2N2O3S
Mol. Mass.:
427.345
SMILES:
CC1CCN(CC1)C(=O)c1cccc(CS(=O)(=O)c2c(Cl)cccc2Cl)n1
Structure:
Search PDB for entries with ligand similarity:
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:
Search PDB for entries with ligand similarity: