7YC1
 
 | | Crystal structure of FGFR4 kinase domain with 10d | | Descriptor: | Fibroblast growth factor receptor 4, GLYCEROL, SULFATE ION, ... | | Authors: | Chen, X.J, Lin, Q.M, Chen, Y.H. | | Deposit date: | 2022-06-30 | | Release date: | 2022-11-16 | | Last modified: | 2024-10-16 | | Method: | X-RAY DIFFRACTION (2.535 Å) | | Cite: | Design, Synthesis, and Biological Evaluation of 5-Formyl-pyrrolo[3,2- b ]pyridine-3-carboxamides as New Selective, Potent, and Reversible-Covalent FGFR4 Inhibitors.
J.Med.Chem., 65, 2022
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7YBP
 | | Crystal structure of FGFR4(V550L) kinase domain with 10z | | Descriptor: | Fibroblast growth factor receptor 4, SULFATE ION, ~{N}-[4-[(1~{R})-1-[3,5-bis(chloranyl)pyridin-4-yl]ethoxy]-5-cyano-pyridin-2-yl]-6-bromanyl-5-(hydroxymethyl)-1-(2-morpholin-4-ylethyl)pyrrolo[3,2-b]pyridine-3-carboxamide | | Authors: | Chen, X.J, Lin, Q.M, Chen, Y.H. | | Deposit date: | 2022-06-29 | | Release date: | 2022-11-16 | | Last modified: | 2024-11-20 | | Method: | X-RAY DIFFRACTION (2.243 Å) | | Cite: | Design, Synthesis, and Biological Evaluation of 5-Formyl-pyrrolo[3,2- b ]pyridine-3-carboxamides as New Selective, Potent, and Reversible-Covalent FGFR4 Inhibitors.
J.Med.Chem., 65, 2022
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7YBX
 | | Crystal structure of FGFR4(V550M) kinase domain with 10z | | Descriptor: | Fibroblast growth factor receptor 4, SULFATE ION, ~{N}-[4-[(1~{R})-1-[3,5-bis(chloranyl)pyridin-4-yl]ethoxy]-5-cyano-pyridin-2-yl]-6-bromanyl-5-(hydroxymethyl)-1-(2-morpholin-4-ylethyl)pyrrolo[3,2-b]pyridine-3-carboxamide | | Authors: | Chen, X.J, Lin, Q.M, Chen, Y.H. | | Deposit date: | 2022-06-30 | | Release date: | 2022-11-16 | | Last modified: | 2024-11-13 | | Method: | X-RAY DIFFRACTION (2.233 Å) | | Cite: | Design, Synthesis, and Biological Evaluation of 5-Formyl-pyrrolo[3,2- b ]pyridine-3-carboxamides as New Selective, Potent, and Reversible-Covalent FGFR4 Inhibitors.
J.Med.Chem., 65, 2022
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7EN0
 | | Structure and Activity of SLAC1 Channels for Stomatal Signaling in Leaves | | Descriptor: | DIUNDECYL PHOSPHATIDYL CHOLINE, SLow Anion Channel 1, SPHINGOSINE | | Authors: | Deng, Y, Kashtoh, H, Wang, Q, Zhen, G, Li, Q, Tang, L, Gao, H, Zhang, C, Qin, L, Su, M, Li, F, Huang, X, Wang, Y, Xie, Q, Clarke, O.B, Hendrickson, W.A, Chen, Y. | | Deposit date: | 2021-04-15 | | Release date: | 2021-05-19 | | Last modified: | 2024-06-05 | | Method: | ELECTRON MICROSCOPY (2.97 Å) | | Cite: | Structure and activity of SLAC1 channels for stomatal signaling in leaves.
Proc.Natl.Acad.Sci.USA, 118, 2021
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7Y4T
 | | Crystal structure of cMET kinase domain bound by compound 9I | | Descriptor: | 2-[2-[3-(1-methylpyrazol-4-yl)quinolin-6-yl]ethyl]-6-(3-nitrophenyl)pyridazin-3-one, Hepatocyte growth factor receptor | | Authors: | Qu, L.Z, Chen, Y.H. | | Deposit date: | 2022-06-16 | | Release date: | 2022-11-23 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.16 Å) | | Cite: | Discovery of D6808, a Highly Selective and Potent Macrocyclic c-Met Inhibitor for Gastric Cancer Harboring MET Gene Alteration Treatment.
J.Med.Chem., 65, 2022
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7Y4U
 | | Crystal structure of cMET kinase domain bound by compound 9Y | | Descriptor: | Hepatocyte growth factor receptor, ~{N}-methyl-4-[1-[2-[3-(1-methylpyrazol-4-yl)quinolin-6-yl]ethyl]-6-oxidanylidene-pyridazin-3-yl]-2-(trifluoromethyl)benzamide | | Authors: | Qu, L.Z, Chen, Y.H. | | Deposit date: | 2022-06-16 | | Release date: | 2022-11-23 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.26 Å) | | Cite: | Discovery of D6808, a Highly Selective and Potent Macrocyclic c-Met Inhibitor for Gastric Cancer Harboring MET Gene Alteration Treatment.
J.Med.Chem., 65, 2022
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7DTZ
 | | FGFR4 complex with a covalent inhibitor | | Descriptor: | Fibroblast growth factor receptor 4, N-[2-[[5-[[2,6-bis(chloranyl)-3,5-dimethoxy-phenyl]methoxy]pyrimidin-2-yl]amino]-3-methyl-phenyl]-2-fluoranyl-prop-2-enamide, SULFATE ION | | Authors: | Chen, X.J, Dai, S.Y, Chen, Y.H. | | Deposit date: | 2021-01-07 | | Release date: | 2021-04-14 | | Last modified: | 2024-10-23 | | Method: | X-RAY DIFFRACTION (2.01 Å) | | Cite: | Investigation of Covalent Warheads in the Design of 2-Aminopyrimidine-based FGFR4 Inhibitors.
Acs Med.Chem.Lett., 12, 2021
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8K79
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8K78
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7D5O
 | | C-Src in complex with TAS-120 | | Descriptor: | 1-[(3S)-3-{4-amino-3-[(3,5-dimethoxyphenyl)ethynyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl}pyrrolidin-1-yl]prop-2-en-1-one, Proto-oncogene tyrosine-protein kinase Src | | Authors: | Qu, L.Z, Chen, Y.H. | | Deposit date: | 2020-09-27 | | Release date: | 2021-12-22 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.69 Å) | | Cite: | Structural insights into the potency and selectivity of covalent pan-FGFR inhibitors
Commun Chem, 5, 2022
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8KH8
 | | Crystal structure of FGFR4(V550L) kinase domain with 8z | | Descriptor: | 1,2-ETHANEDIOL, 1-[4-[(1~{R})-1-[3,5-bis(chloranyl)pyridin-4-yl]ethoxy]-5-cyano-pyridin-2-yl]-3-[6-methanoyl-5-[(4-methyl-2-oxidanylidene-piperazin-1-yl)methyl]-3-(2-morpholin-4-ylethoxy)pyridin-2-yl]urea, Fibroblast growth factor receptor 4, ... | | Authors: | Lin, Q.M, Chen, X.J, Chen, Y.H. | | Deposit date: | 2023-08-21 | | Release date: | 2024-07-31 | | Last modified: | 2024-11-20 | | Method: | X-RAY DIFFRACTION (1.49 Å) | | Cite: | Discovery of 6-Formylpyridyl Urea Derivatives as Potent Reversible-Covalent Fibroblast Growth Factor Receptor 4 Inhibitors with Improved Anti-Hepatocellular Carcinoma Activity.
J.Med.Chem., 67, 2024
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8KH6
 | | Crystal structure of FGFR4 kinase domain with 8r | | Descriptor: | 1,2-ETHANEDIOL, 1-[4-[(1~{R})-1-[3,5-bis(chloranyl)pyridin-4-yl]ethoxy]-5-cyano-pyridin-2-yl]-3-[5-bromanyl-6-(hydroxymethyl)-3-methoxy-pyridin-2-yl]urea, Fibroblast growth factor receptor 4, ... | | Authors: | Lin, Q.M, Chen, X.J, Chen, Y.H. | | Deposit date: | 2023-08-21 | | Release date: | 2024-07-31 | | Last modified: | 2024-11-13 | | Method: | X-RAY DIFFRACTION (1.62 Å) | | Cite: | Discovery of 6-Formylpyridyl Urea Derivatives as Potent Reversible-Covalent Fibroblast Growth Factor Receptor 4 Inhibitors with Improved Anti-Hepatocellular Carcinoma Activity.
J.Med.Chem., 67, 2024
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8KH9
 | | Crystal structure of FGFR4(V550M) kinase domain with 8z | | Descriptor: | 1,2-ETHANEDIOL, 1-[4-[(1~{R})-1-[3,5-bis(chloranyl)pyridin-4-yl]ethoxy]-5-cyano-pyridin-2-yl]-3-[6-methanoyl-5-[(4-methyl-2-oxidanylidene-piperazin-1-yl)methyl]-3-(2-morpholin-4-ylethoxy)pyridin-2-yl]urea, Fibroblast growth factor receptor 4, ... | | Authors: | Lin, Q.M, Chen, X.J, Chen, Y.H. | | Deposit date: | 2023-08-21 | | Release date: | 2024-07-31 | | Last modified: | 2024-10-23 | | Method: | X-RAY DIFFRACTION (1.42 Å) | | Cite: | Discovery of 6-Formylpyridyl Urea Derivatives as Potent Reversible-Covalent Fibroblast Growth Factor Receptor 4 Inhibitors with Improved Anti-Hepatocellular Carcinoma Activity.
J.Med.Chem., 67, 2024
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8KH7
 | | Crystal structure of FGFR4 kinase domain with 8zc | | Descriptor: | 1,2-ETHANEDIOL, 1-[4-[(1~{R})-1-[3,5-bis(chloranyl)pyridin-4-yl]ethoxy]-5-cyano-pyridin-2-yl]-3-[6-methanoyl-5-[(4-methyl-2-oxidanylidene-piperazin-1-yl)methyl]-3-(2-morpholin-4-ylethoxy)pyridin-2-yl]urea, Fibroblast growth factor receptor 4, ... | | Authors: | Lin, Q.M, Chen, X.J, Chen, Y.H. | | Deposit date: | 2023-08-21 | | Release date: | 2024-07-31 | | Last modified: | 2024-11-06 | | Method: | X-RAY DIFFRACTION (1.52 Å) | | Cite: | Discovery of 6-Formylpyridyl Urea Derivatives as Potent Reversible-Covalent Fibroblast Growth Factor Receptor 4 Inhibitors with Improved Anti-Hepatocellular Carcinoma Activity.
J.Med.Chem., 67, 2024
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7CBY
 | | Structure of FOXG1 DNA binding domain bound to DBE2 DNA site | | Descriptor: | DI(HYDROXYETHYL)ETHER, DNA (5'-D(*CP*AP*AP*AP*AP*TP*GP*TP*AP*AP*AP*CP*AP*AP*GP*A)-3'), DNA (5'-D(*TP*CP*TP*TP*GP*TP*TP*TP*AP*CP*AP*TP*TP*TP*TP*G)-3'), ... | | Authors: | Dai, S.Y, Li, J, Chen, Y.H. | | Deposit date: | 2020-06-15 | | Release date: | 2020-10-28 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (1.646 Å) | | Cite: | Structural Basis for DNA Recognition by FOXG1 and the Characterization of Disease-causing FOXG1 Mutations.
J.Mol.Biol., 432, 2020
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8JOT
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8JMZ
 | | FGFR1 kinase domain with sulfatinib | | Descriptor: | Fibroblast growth factor receptor 1, GLYCEROL, SULFATE ION, ... | | Authors: | Chen, X.J, Lin, Q.M, Chen, Y.H. | | Deposit date: | 2023-06-05 | | Release date: | 2024-03-27 | | Last modified: | 2024-11-20 | | Method: | X-RAY DIFFRACTION (1.988 Å) | | Cite: | Structural basis and selectivity of sulfatinib binding to FGFR and CSF-1R.
Commun Chem, 7, 2024
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8XLO
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8XLQ
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8Y22
 | | FGFR1 kinase domain with a covalent inhibitor 9g | | Descriptor: | Fibroblast growth factor receptor 1, SULFATE ION, ~{N}-[4-[[4-azanyl-3-(7-methoxy-5-methyl-1-benzothiophen-2-yl)pyrazolo[3,4-d]pyrimidin-1-yl]methyl]phenyl]propanamide | | Authors: | Chen, X.J, Chen, Y.H. | | Deposit date: | 2024-01-25 | | Release date: | 2024-06-26 | | Last modified: | 2024-10-30 | | Method: | X-RAY DIFFRACTION (2.792 Å) | | Cite: | Design, synthesis and biological evaluation of 5-amino-1H-pyrazole-4-carboxamide derivatives as pan-FGFR covalent inhibitors.
Eur.J.Med.Chem., 275, 2024
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8XZ7
 | | FGFR1 kinase domain with a covalent inhibitor 10h | | Descriptor: | 5-azanyl-3-[2-[4,6-bis(fluoranyl)-2-methyl-3~{H}-benzimidazol-5-yl]ethynyl]-1-[[3-(prop-2-enoylamino)phenyl]methyl]pyrazole-4-carboxamide, Fibroblast growth factor receptor 1, SULFATE ION | | Authors: | Chen, X.J, Chen, Y.H. | | Deposit date: | 2024-01-20 | | Release date: | 2024-06-26 | | Last modified: | 2024-11-20 | | Method: | X-RAY DIFFRACTION (1.75 Å) | | Cite: | Design, synthesis and biological evaluation of 5-amino-1H-pyrazole-4-carboxamide derivatives as pan-FGFR covalent inhibitors.
Eur.J.Med.Chem., 275, 2024
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7WCX
 | | Crystal structure of FGFR4(V550M) kinase domain with 7v | | Descriptor: | Fibroblast growth factor receptor 4, SULFATE ION, ~{N}-[2-[[5-[(1~{R})-1-[3,5-bis(chloranyl)pyridin-4-yl]ethoxy]-1~{H}-indazol-3-yl]amino]-3-fluoranyl-5-(4-morpholin-4-ylpiperidin-1-yl)phenyl]propanamide | | Authors: | Chen, X.J, Lin, Q.M, Dai, S.Y, Chen, Y.H. | | Deposit date: | 2021-12-20 | | Release date: | 2022-03-30 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.175 Å) | | Cite: | Design, Synthesis, and Biological Evaluation of Aminoindazole Derivatives as Highly Selective Covalent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR4.
J.Med.Chem., 65, 2022
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7WCT
 | | Crystal structure of FGFR4 kinase domain with 7v | | Descriptor: | Fibroblast growth factor receptor 4, GLYCEROL, SULFATE ION, ... | | Authors: | Chen, X.J, Lin, Q.M, Dai, S.Y, Chen, Y.H. | | Deposit date: | 2021-12-20 | | Release date: | 2022-03-30 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.106 Å) | | Cite: | Design, Synthesis, and Biological Evaluation of Aminoindazole Derivatives as Highly Selective Covalent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR4.
J.Med.Chem., 65, 2022
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7WCW
 | | Crystal structure of FGFR4(V550L) kinase domain with 7v | | Descriptor: | Fibroblast growth factor receptor 4, SULFATE ION, ~{N}-[2-[[5-[(1~{R})-1-[3,5-bis(chloranyl)pyridin-4-yl]ethoxy]-1~{H}-indazol-3-yl]amino]-3-fluoranyl-5-(4-morpholin-4-ylpiperidin-1-yl)phenyl]propanamide | | Authors: | Chen, X.J, Lin, Q.M, Dai, S.Y, Chen, Y.H. | | Deposit date: | 2021-12-20 | | Release date: | 2022-03-30 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.317 Å) | | Cite: | Design, Synthesis, and Biological Evaluation of Aminoindazole Derivatives as Highly Selective Covalent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR4.
J.Med.Chem., 65, 2022
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7WCL
 | | Crystal structure of FGFR1 kinase domain with Pemigatinib | | Descriptor: | 11-[2,6-bis(fluoranyl)-3,5-dimethoxy-phenyl]-13-ethyl-4-(morpholin-4-ylmethyl)-5,7,11,13-tetrazatricyclo[7.4.0.0^{2,6}]trideca-1(9),2(6),3,7-tetraen-12-one, Fibroblast growth factor receptor 1, SULFATE ION | | Authors: | Chen, X.J, Lin, Q.M, Jiang, L.Y, Qu, L.Z, Chen, Y.H. | | Deposit date: | 2021-12-20 | | Release date: | 2022-09-14 | | Last modified: | 2023-11-29 | | Method: | X-RAY DIFFRACTION (2.495 Å) | | Cite: | Characterization of the cholangiocarcinoma drug pemigatinib against FGFR gatekeeper mutants.
Commun Chem, 5, 2022
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