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PDBsum entry 5bq0

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Transferase/transferase inhibitor PDB id
5bq0
Contents
Protein chain
265 a.a.
Ligands
4US
DMS
EDO ×2
Waters ×304

References listed in PDB file
Key reference
Title Design and synthesis of carbazole carboxamides as promising inhibitors of bruton'S tyrosine kinase (btk) and janus kinase 2 (jak2).
Authors Q.Liu, D.G.Batt, J.S.Lippy, N.Surti, A.J.Tebben, J.K.Muckelbauer, L.Chen, Y.An, C.Chang, M.Pokross, Z.Yang, H.Wang, J.R.Burke, P.H.Carter, J.A.Tino.
Ref. Bioorg Med Chem Lett, 2015, 25, 4265-4269. [DOI no: 10.1016/j.bmcl.2015.07.102]
PubMed id 26320619
Abstract
Four series of disubstituted carbazole-1-carboxamides were designed and synthesised as inhibitors of Bruton's tyrosine kinase (BTK). 4,7- and 4,6-disubstituted carbazole-1-carboxamides were potent and selective inhibitors of BTK, while 3,7- and 3,6-disubstituted carbazole-1-carboxamides were potent and selective inhibitors of Janus kinase 2 (JAK2).
PROCHECK
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