5TBW
 
 | | Crystal structure of chlorolissoclimide bound to the yeast 80S ribosome | | Descriptor: | 18S ribosomal RNA, 25S ribosomal RNA, 40S ribosomal protein S0-A, ... | | Authors: | Konst, Z.A, Szklarski, A.R, Pellegrino, S, Michalak, S.E, Meyer, M, Zanette, C, Cencic, R, Nam, S, Horne, D.A, Pelletier, J, Mobley, D.L, Yusupova, G, Yusupov, M, Vanderwal, C.D. | | Deposit date: | 2016-09-13 | | Release date: | 2017-07-26 | | Last modified: | 2024-01-17 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Synthesis facilitates an understanding of the structural basis for translation inhibition by the lissoclimides.
Nat Chem, 9, 2017
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6HHQ
 | | Crystal structure of compound C45 bound to the yeast 80S ribosome | | Descriptor: | (3~{R})-3-[(1~{S})-2-[(1~{S},4~{a}~{R},6~{S},7~{S},8~{a}~{R})-6,7-bis(chloranyl)-5,5,8~{a}-trimethyl-2-methylidene-3,4,4~{a},6,7,8-hexahydro-1~{H}-naphthalen-1-yl]-1-oxidanyl-ethyl]pyrrolidine-2,5-dione, 18S ribosomal RNA, 25S ribosomal RNA, ... | | Authors: | Pellegrino, S, Vanderwal, C.D, Yusupov, M. | | Deposit date: | 2018-08-28 | | Release date: | 2019-02-20 | | Last modified: | 2024-05-15 | | Method: | X-RAY DIFFRACTION (3.10000038 Å) | | Cite: | Understanding the role of intermolecular interactions between lissoclimides and the eukaryotic ribosome.
Nucleic Acids Res., 47, 2019
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8U2E
 | | Bruton's tyrosine kinase in complex with N-[(2R)-1-[(3R)-3-(methylcarbamoyl)-1H,2H,3H,4H,9H-pyrido[3,4-b]indol-2-yl]-3-(3-methylphenyl)-1-oxopropan-2-yl]-1H-indazole-5-carboxamide | | Descriptor: | (2S)-6-fluoro-5-[(3S)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]-2-(4-methylpiperazine-1-carbonyl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide, 1,2-ETHANEDIOL, CHLORIDE ION, ... | | Authors: | Gajewski, S, Clifton, M.C. | | Deposit date: | 2023-09-05 | | Release date: | 2024-01-31 | | Last modified: | 2024-03-06 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Discovery and Preclinical Pharmacology of NX-2127, an Orally Bioavailable Degrader of Bruton's Tyrosine Kinase with Immunomodulatory Activity for the Treatment of Patients with B Cell Malignancies.
J.Med.Chem., 67, 2024
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8U2D
 | | Bruton's tyrosine kinase in complex with N-[(2R)-1-[(3R)-3-(methylcarbamoyl)-1H,2H,3H,4H,9H-pyrido[3,4-b]indol-2-yl]-3-(3-methylphenyl)-1-oxopropan-2-yl]-1H-indazole-5-carboxamide | | Descriptor: | (3R)-2-[N-(1H-indazole-5-carbonyl)-3-methyl-D-phenylalanyl]-N-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxamide, 1,2-ETHANEDIOL, CHLORIDE ION, ... | | Authors: | Gajewski, S, Clifton, M.C. | | Deposit date: | 2023-09-05 | | Release date: | 2024-01-31 | | Last modified: | 2024-03-06 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Discovery and Preclinical Pharmacology of NX-2127, an Orally Bioavailable Degrader of Bruton's Tyrosine Kinase with Immunomodulatory Activity for the Treatment of Patients with B Cell Malignancies.
J.Med.Chem., 67, 2024
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9D3V
 | | CRYSTAL STRUCTURE OF EGFR(L858R/T790M/C797S) IN COMPLEX WITH AUR-3418 | | Descriptor: | (4S)-N-[2-(4-methoxypiperidin-1-yl)pyrimidin-4-yl]-2-methyl-1-(propan-2-yl)-1H-imidazo[1,2-b]pyrazol-6-amine, CHLORIDE ION, Epidermal growth factor receptor | | Authors: | Bell, J.A. | | Deposit date: | 2024-08-12 | | Release date: | 2025-03-05 | | Method: | X-RAY DIFFRACTION (2.32 Å) | | Cite: | Discovery of a Novel Mutant-Selective Epidermal Growth Factor Receptor Inhibitor Using an In Silico Enabled Drug Discovery Platform.
J.Med.Chem., 67, 2024
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9D3W
 | | CRYSTAL STRUCTURE OF EGFR(L858R/T790M/C797S) IN COMPLEX WITH AUR-8250 | | Descriptor: | (4S)-1-(1,4-dioxaspiro[4.5]decan-8-yl)-N-{2-[(3S,4R)-3-fluoro-4-methoxypiperidin-1-yl]pyrimidin-4-yl}-2-methyl-1H-imidazo[1,2-b]pyrazol-6-amine, CHLORIDE ION, Epidermal growth factor receptor | | Authors: | Bell, J.A. | | Deposit date: | 2024-08-12 | | Release date: | 2025-03-05 | | Method: | X-RAY DIFFRACTION (2.53 Å) | | Cite: | Discovery of a Novel Mutant-Selective Epidermal Growth Factor Receptor Inhibitor Using an In Silico Enabled Drug Discovery Platform.
J.Med.Chem., 67, 2024
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