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PDBsum entry 4id7
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Transferase/transferase inhibitor
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PDB id
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4id7
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References listed in PDB file
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Key reference
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Title
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Discovery of potent, Selective and orally bioavailable imidazo[1,5-A]pyrazine derived ack1 inhibitors.
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Authors
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M.Jin,
J.Wang,
A.Kleinberg,
M.Kadalbajoo,
K.W.Siu,
A.Cooke,
M.A.Bittner,
Y.Yao,
A.Thelemann,
Q.Ji,
S.Bhagwat,
K.M.Mulvihill,
J.A.Rechka,
J.A.Pachter,
A.P.Crew,
D.Epstein,
M.J.Mulvihill.
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Ref.
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Bioorg Med Chem Lett, 2013,
23,
979-984.
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PubMed id
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Abstract
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This Letter describes the medicinal chemistry effort towards a series of novel
imidazo[1,5-a]pyrazine derived inhibitors of ACK1. Virtual screening led to the
discovery of the initial hit, and subsequent exploration of structure-activity
relationships and optimization of drug metabolism and pharmacokinetic properties
led to the identification of potent, selective and orally bioavailable ACK1
inhibitors.
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