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TitleDiscovery of SAR184841, a potent and long-lasting inhibitor of 11beta-hydroxysteroid dehydrogenase type 1, active in a physiopathological animal model of T2D
Journal, issue, pagesBioorg. Med. Chem. Lett., Vol. 23, Page 2414-2421, Year 2013
Publish dateNov 9, 2012 (structure data deposition date)
AuthorsVenier, O. / Pascal, C. / Braun, A. / Namane, C. / Mougenot, P. / Crespin, O. / Pacquet, F. / Mougenot, C. / Monseau, C. / Onofri, B. ...Venier, O. / Pascal, C. / Braun, A. / Namane, C. / Mougenot, P. / Crespin, O. / Pacquet, F. / Mougenot, C. / Monseau, C. / Onofri, B. / Dadji-Faihun, R. / Leger, C. / Ben-Hassine, M. / Van-Pham, T. / Ragot, J.L. / Philippo, C. / Farjot, G. / Noah, L. / Maniani, K. / Boutarfa, A. / Nicolai, E. / Guillot, E. / Pruniaux, M.P. / Gussregen, S. / Engel, C. / Coutant, A.L. / de Miguel, B. / Castro, A.
External linksBioorg. Med. Chem. Lett. / PubMed:23478147
MethodsX-ray diffraction
Resolution2.19 Å
Structure data

PDB-4hx5:
Crystal structure of 11 beta-HSD1 in complex with SAR184841
Method: X-RAY DIFFRACTION / Resolution: 2.19 Å

Chemicals

ChemComp-19V:
4-[5-(4-tert-butylpiperazin-1-yl)pyridin-2-yl]-N-[(1R,2S,3S,5S,7s)-5-carbamoyltricyclo[3.3.1.1~3,7~]dec-2-yl]-3,4-dihydroquinoxaline-1(2H)-carboxamide

ChemComp-NDP:
NADPH DIHYDRO-NICOTINAMIDE-ADENINE-DINUCLEOTIDE PHOSPHATE

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsOXIDOREDUCTASE/OXIDOREDUCTASE INHIBITOR / 11BETA / HYDROXYSTEROID / DEHYDROGENASE / OXIDOREDUCTASE-OXIDOREDUCTASE INHIBITOR COMPLEX

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