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3T9I
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BU of 3t9i by Molmil
Pim1 complexed with a novel 3,6-disubstituted indole at 2.6 Ang Resolution
Descriptor: 2-methoxy-4-(3-phenyl-2H-pyrazolo[3,4-b]pyridin-6-yl)phenol, Proto-oncogene serine/threonine-protein kinase pim-1
Authors:Bellamacina, C, Shu, W, Le, V, Nishiguchi, G, Bussiere, D.
Deposit date:2011-08-02
Release date:2011-10-12
Last modified:2024-11-06
Method:X-RAY DIFFRACTION (2.6 Å)
Cite:Discovery of novel 3,5-disubstituted indole derivatives as potent inhibitors of Pim-1, Pim-2, and Pim-3 protein kinases.
Bioorg.Med.Chem.Lett., 21, 2011
5DWR
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BU of 5dwr by Molmil
Identification of N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1,2 and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies
Descriptor: N-{4-[(1R,3S,5S)-3-amino-5-methylcyclohexyl]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide, Serine/threonine-protein kinase pim-1
Authors:Bellamacina, C, Bussiere, D, Burger, M.
Deposit date:2015-09-22
Release date:2015-11-11
Last modified:2024-10-16
Method:X-RAY DIFFRACTION (2 Å)
Cite:Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies.
J.Med.Chem., 58, 2015
6WWB
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BU of 6wwb by Molmil
Crystal Structure of the second bromodomain of human BRD2 in complex with the compound 3b
Descriptor: 1,2-ETHANEDIOL, 2-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-((1-(4-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)acetamido)butyl)-1H-1,2,3-triazol-4-yl)methyl)acetamide, Bromodomain-containing protein 2
Authors:White, S.W, Yun, M.
Deposit date:2020-05-08
Release date:2021-11-17
Last modified:2023-10-18
Method:X-RAY DIFFRACTION (1.31 Å)
Cite:Phenyl-Glutarimides: Alternative Cereblon Binders for the Design of PROTACs.
Angew.Chem.Int.Ed.Engl., 60, 2021
7SHH
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BU of 7shh by Molmil
Bacterial cereblon homologue in complex with (R)-3-(4-methoxyphenyl)piperidine-2,6-dione
Descriptor: (3R)-3-(4-methoxyphenyl)piperidine-2,6-dione, Cereblon isoform 4, ZINC ION
Authors:Nithianantham, S, Fischer, M.
Deposit date:2021-10-08
Release date:2022-04-13
Last modified:2024-05-22
Method:X-RAY DIFFRACTION (1.9 Å)
Cite:Development of Potent and Selective Janus Kinase 2/3 Directing PG-PROTACs.
Acs Med.Chem.Lett., 13, 2022
4N70
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BU of 4n70 by Molmil
Pim1 Complexed with a pyridylcarboxamide
Descriptor: N-{4-[(3R,4R,5S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl]pyridin-3-yl}-6-(2,6-difluorophenyl)-5-fluoropyridine-2-carboxamide, Serine/threonine-protein kinase pim-1
Authors:Bellamacina, C.R, Le, V, Shu, W, Burger, M.T, Bussiere, D.
Deposit date:2013-10-14
Release date:2013-11-06
Last modified:2024-10-30
Method:X-RAY DIFFRACTION (2.1 Å)
Cite:Structure Guided Optimization, in Vitro Activity, and in Vivo Activity of Pan-PIM Kinase Inhibitors.
ACS Med Chem Lett, 4, 2013
4N6Y
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BU of 4n6y by Molmil
Pim1 Complexed with a phenylcarboxamide
Descriptor: 2-(acetylamino)-N-[2-(piperidin-1-yl)phenyl]-1,3-thiazole-4-carboxamide, Serine/threonine-protein kinase pim-1
Authors:Bellamacina, C.R, Le, V, Shu, W, Burger, M.T, Bussiere, D.
Deposit date:2013-10-14
Release date:2013-11-06
Last modified:2024-11-06
Method:X-RAY DIFFRACTION (2.6 Å)
Cite:Structure Guided Optimization, in Vitro Activity, and in Vivo Activity of Pan-PIM Kinase Inhibitors.
ACS Med Chem Lett, 4, 2013
4N6Z
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BU of 4n6z by Molmil
Pim1 Complexed with a pyridylcarboxamide
Descriptor: 3-amino-N-{4-[(3S)-3-aminopiperidin-1-yl]pyridin-3-yl}pyrazine-2-carboxamide, GLYCEROL, Serine/threonine-protein kinase pim-1
Authors:Bellamacina, C.R, Le, V, Shu, W, Burger, M.T, Bussiere, D.
Deposit date:2013-10-14
Release date:2013-11-06
Last modified:2014-07-02
Method:X-RAY DIFFRACTION (2.2 Å)
Cite:Structure Guided Optimization, in Vitro Activity, and in Vivo Activity of Pan-PIM Kinase Inhibitors.
ACS Med Chem Lett, 4, 2013

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數據於2024-11-06公開中

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