4AOF
 
 | | Selective small molecule inhibitor discovered by chemoproteomic assay platform reveals regulation of Th17 cell differentiation by PI3Kgamma | | 分子名称: | N-[6-(5-methylsulfonylpyridin-3-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl]ethanamide, PHOSPHATIDYLINOSITOL-4,5-BISPHOSPHATE 3-KINASE CATALYTIC SUBUNIT GAMMA ISOFORM | | 著者 | Bergamini, G, Bell, K, Shimamura, S, Werner, T, Cansfield, A, Muller, K, Perrin, J, Rau, C, Ellard, K, Hopf, C, Doce, C, Leggate, D, Mangano, R, Mathieson, T, OMahony, A, Plavec, I, Rharbaoui, F, Reinhard, F, Savitski, M.M, Ramsden, N, Hirsch, E, Drewes, G, Rausch, O, Bantscheff, M, Neubauer, G. | | 登録日 | 2012-03-26 | | 公開日 | 2012-05-09 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (3.3 Å) | | 主引用文献 | A Selective Inhibitor Reveals Pi3Kgamma Dependence of T(H)17 Cell Differentiation.
Nat.Chem.Biol., 8, 2012
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4HYF
 | | Structural basis and SAR for OD 270, a lead stage 1,2,4-triazole based specific Tankyrase1/2 inhibitor | | 分子名称: | 4-{5-[(E)-2-{4-(2-chlorophenyl)-5-[5-(methylsulfonyl)pyridin-2-yl]-4H-1,2,4-triazol-3-yl}ethenyl]-1,3,4-oxadiazol-2-yl}benzonitrile, NICOTINAMIDE, Tankyrase-2, ... | | 著者 | Perdreau, H, Ekblad, B, Voronkov, A, Holsworth, D.D, Waaler, J, Drewes, G, Schueler, H, Krauss, S, Morth, J.P. | | 登録日 | 2012-11-13 | | 公開日 | 2013-03-20 | | 最終更新日 | 2023-09-20 | | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | | 主引用文献 | Structural Basis and SAR for G007-LK, a Lead Stage 1,2,4-Triazole Based Specific Tankyrase 1/2 Inhibitor.
J.Med.Chem., 56, 2013
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4CFK
 | | N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH LY294002 | | 分子名称: | 1,2-ETHANEDIOL, 2-MORPHOLIN-4-YL-7-PHENYL-4H-CHROMEN-4-ONE, BRD4 PROTEIN, ... | | 著者 | Chung, C, Dittmann, A, Drewes, G. | | 登録日 | 2013-11-18 | | 公開日 | 2014-01-15 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (1.55 Å) | | 主引用文献 | The Commonly Used Pi3-Kinase Probe Ly294002 is an Inhibitor of Bet Bromodomains.
Acs Chem.Biol., 9, 2014
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4CFL
 | | N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH LY303511 | | 分子名称: | 1,2-ETHANEDIOL, 8-phenyl-2-piperazin-1-yl-chromen-4-one, BRD4 PROTEIN, ... | | 著者 | Chung, C, Dittmann, A, Drewes, G. | | 登録日 | 2013-11-18 | | 公開日 | 2014-01-15 | | 最終更新日 | 2024-05-08 | | 実験手法 | X-RAY DIFFRACTION (1.32 Å) | | 主引用文献 | The Commonly Used Pi3-Kinase Probe Ly294002 is an Inhibitor of Bet Bromodomains.
Acs Chem.Biol., 9, 2014
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3ZYU
 | | Crystal Structure of the first bromodomain of human BRD4 in complex with I-BET151(GSK1210151A) | | 分子名称: | 1,2-ETHANEDIOL, 7-(3,5-DIMETHYL-1,2-OXAZOL-4-YL)-8-METHOXY-1-[(1R)-1-(PYRIDIN-2-YL)ETHYL]-1H,2H,3H-IMIDAZO[4,5-C]QUINOLIN-2-ONE, BROMODOMAIN-CONTAINING PROTEIN 4 | | 著者 | Chung, C.W, Mirguet, O. | | 登録日 | 2011-08-25 | | 公開日 | 2011-11-02 | | 最終更新日 | 2023-12-20 | | 実験手法 | X-RAY DIFFRACTION (1.5 Å) | | 主引用文献 | Inhibition of Bet Recruitment to Chromatin as an Effective Treatment for Mll-Fusion Leukaemia.
Nature, 478, 2011
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