6IAR
 
 | | Tricyclic indazoles a novel class of selective estrogen receptor degrader antagonists | | Descriptor: | 3-[4-[(6~{R})-7-(2-methylpropyl)-3,6,8,9-tetrahydropyrazolo[4,3-f]isoquinolin-6-yl]phenyl]propanoic acid, Estrogen receptor | | Authors: | Scott, J.S, Bailey, A, Buttar, D, Carbajo, R.J, Curwen, J, Davies, R.D.M, Degorce, S.L, Donald, C, Gangl, E, Greenwood, R, Groombridge, S.D, Johnson, T, Lamont, S, Lawson, M, Lister, A, Morrow, C, Moss, T, Pink, J.H, Polanski, R. | | Deposit date: | 2018-11-27 | | Release date: | 2019-01-23 | | Last modified: | 2024-05-15 | | Method: | X-RAY DIFFRACTION (1.84 Å) | | Cite: | Tricyclic Indazoles-A Novel Class of Selective Estrogen Receptor Degrader Antagonists.
J.Med.Chem., 62, 2019
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5FXS
 | | IGFR-1R complex with a pyrimidine inhibitor. | | Descriptor: | 2-[4-[4-[[(6Z)-5-chloranyl-6-pyrazolo[1,5-a]pyridin-3-ylidene-1H-pyrimidin-2-yl]amino]-3,5-dimethyl-pyrazol-1-yl]piperidin-1-yl]-N,N-dimethyl-ethanamide, ACETATE ION, INSULIN-LIKE GROWTH FACTOR 1 RECEPTOR | | Authors: | Degorce, S, Boyd, S, Curwen, J, Ducray, R, Halsall, C, Jones, C, Lach, F, Lenz, E, Pass, M, Pass, S, Trigwell, C, Norman, R, Phillips, C. | | Deposit date: | 2016-03-02 | | Release date: | 2016-10-19 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Discovery of a Potent, Selective, Orally Bioavailable, and Efficacious Novel 2-(Pyrazol-4-ylamino)-pyrimidine Inhibitor of the Insulin-like Growth Factor-1 Receptor (IGF-1R).
J. Med. Chem., 59, 2016
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5FXQ
 | | IGFR-1R complex with a pyrimidine inhibitor. | | Descriptor: | 5-chloranyl-4-imidazo[1,2-a]pyridin-3-yl-N-(5-methyl-1-piperidin-4-yl-pyrazol-4-yl)pyrimidin-2-amine, INSULIN-LIKE GROWTH FACTOR 1 RECEPTOR | | Authors: | Degorce, S, Boyd, S, Curwen, J, Ducray, R, Halsall, C, Jones, C, Lach, F, Lenz, E, Pass, M, Pass, S, Trigwell, C, Norman, R, Phillips, C. | | Deposit date: | 2016-03-02 | | Release date: | 2016-10-19 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Discovery of a Potent, Selective, Orally Bioavailable, and Efficacious Novel 2-(Pyrazol-4-ylamino)-pyrimidine Inhibitor of the Insulin-like Growth Factor-1 Receptor (IGF-1R).
J. Med. Chem., 59, 2016
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5FXR
 | | IGFR-1R complex with a pyrimidine inhibitor. | | Descriptor: | 5-chloranyl-4-imidazo[1,2-a]pyridin-3-yl-N-(3-methyl-1-piperidin-4-yl-pyrazol-4-yl)pyrimidin-2-amine, INSULIN-LIKE GROWTH FACTOR 1 RECEPTOR | | Authors: | Degorce, S, Boyd, S, Curwen, J, Ducray, R, Halsall, C, Jones, C, Lach, F, Lenz, E, Pass, M, Pass, S, Trigwell, C, Norman, R, Phillips, C. | | Deposit date: | 2016-03-02 | | Release date: | 2016-10-19 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Discovery of a Potent, Selective, Orally Bioavailable, and Efficacious Novel 2-(Pyrazol-4-ylamino)-pyrimidine Inhibitor of the Insulin-like Growth Factor-1 Receptor (IGF-1R).
J. Med. Chem., 59, 2016
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2H8H
 | | Src kinase in complex with a quinazoline inhibitor | | Descriptor: | N-(5-CHLORO-1,3-BENZODIOXOL-4-YL)-7-[2-(4-METHYLPIPERAZIN-1-YL)ETHOXY]-5-(TETRAHYDRO-2H-PYRAN-4-YLOXY)QUINAZOLIN-4-AMINE, Proto-oncogene tyrosine-protein kinase Src | | Authors: | Otterbein, L.R, Norman, R, Pauptit, R.A, Rowsell, S, Breed, J. | | Deposit date: | 2006-06-07 | | Release date: | 2006-11-21 | | Last modified: | 2024-10-30 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.
J.Med.Chem., 49, 2006
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2WQB
 | | Structure of the Tie2 kinase domain in complex with a thiazolopyrimidine inhibitor | | Descriptor: | 2-[3-(CYCLOHEXYLMETHYL)-5-PHENYL-IMIDAZOL-4-YL]-[1,3]THIAZOLO[4,5-E]PYRIMIDIN-7-AMINE, ANGIOPOIETIN-1 RECEPTOR | | Authors: | Brassington, C, Breed, J, Buttar, D, Fitzek, M, Forder, C, Hassall, L, Hayter, B.R, Jones, C.D, Luke, R.W.A, McCall, E, McCoull, W, Norman, R, Paterson, D, McMiken, H, Rowsell, S, Tucker, J.A. | | Deposit date: | 2009-08-18 | | Release date: | 2009-11-03 | | Last modified: | 2024-11-13 | | Method: | X-RAY DIFFRACTION (2.95 Å) | | Cite: | Novel Thienopyrimidine and Thiazolopyrimidine Kinase Inhibitors with Activity Against Tie-2 in Vitro and in Vivo.
Bioorg.Med.Chem.Lett., 19, 2009
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