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PDBsum entry 5aep
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References listed in PDB file
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Key reference
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Title
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Novel pyrrole carboxamide inhibitors of jak2 as potential treatment of myeloproliferative disorders.
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Authors
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M.G.Brasca,
P.Gnocchi,
M.Nesi,
N.Amboldi,
N.Avanzi,
J.Bertrand,
S.Bindi,
G.Canevari,
D.Casero,
M.Ciomei,
N.Colombo,
S.Cribioli,
G.Fachin,
E.R.Felder,
A.Galvani,
A.Isacchi,
I.Motto,
A.Panzeri,
D.Donati.
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Ref.
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Bioorg Med Chem Lett, 2015,
23,
2387-2407.
[DOI no: ]
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PubMed id
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Abstract
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Compound 1, a hit from the screening of our chemical collection displaying
activity against JAK2, was deconstructed for SAR analysis into three regions,
which were explored. A series of compounds was synthesized leading to the
identification of the potent and orally bioavailable JAK2 inhibitor 16
(NMS-P830), which showed an encouraging tumour growth inhibition in SET-2
xenograft tumour model, with evidence for JAK2 pathway suppression demonstrated
by in vivo pharmacodynamic effects.
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