3V4A
 
 | | Structure of ar lbd with activator peptide and sarm inhibitor 2 | | Descriptor: | (5R)-3-(3,4-dichlorophenyl)-5-(4-hydroxyphenyl)-1,5-dimethyl-2-thioxoimidazolidin-4-one, Androgen receptor, SULFATE ION | | Authors: | Nique, F, Hebbe, S, Peixoto, C, Annoot, D, Lefrancois, J.-M, Duval, E, Michoux, L, Triballeau, N, Lemoullec, J.M, Mollat, P, Thauvin, M, Prange, T, Minet, D, Clement-Lacroix, P, Robin-Jagerschmidt, C, Fleury, D, Guedin, D, Deprez, P. | | Deposit date: | 2011-12-14 | | Release date: | 2012-09-05 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Discovery of diarylhydantoins as new selective androgen receptor modulators.
J.Med.Chem., 55, 2012
|
|
3V49
 | | Structure of ar lbd with activator peptide and sarm inhibitor 1 | | Descriptor: | 4-[(4R)-4-(4-hydroxyphenyl)-3,4-dimethyl-2,5-dioxoimidazolidin-1-yl]-2-(trifluoromethyl)benzonitrile, Androgen receptor, activator peptide, ... | | Authors: | Nique, F, Hebbe, S, Peixoto, C, Annoot, D, Lefrancois, J.-M, Duval, E, Michoux, L, Triballeau, N, Lemoullec, J.-M, Mollat, P, Thauvin, M, Prange, T, Minet, D, Clement-Lacroix, P, Robin-Jagerschmidt, C, Fleury, D, Guedin, D, Deprez, P. | | Deposit date: | 2011-12-14 | | Release date: | 2012-09-05 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | Discovery of diarylhydantoins as new selective androgen receptor modulators.
J.Med.Chem., 55, 2012
|
|
1KZN
 | | Crystal Structure of E. coli 24kDa Domain in Complex with Clorobiocin | | Descriptor: | CLOROBIOCIN, DNA GYRASE SUBUNIT B | | Authors: | Lafitte, D, Lamour, V, Tsvetkov, P.O, Makarov, A.A, Klich, M, Deprez, P, Moras, D, Briand, C, Gilli, R. | | Deposit date: | 2002-02-07 | | Release date: | 2002-06-19 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | DNA gyrase interaction with coumarin-based inhibitors: the role of the hydroxybenzoate isopentenyl moiety and the 5'-methyl group of the noviose.
Biochemistry, 41, 2002
|
|
6YJM
 | | Crystal Structure of the Catalytic Domain of ADAMTS-5 in Complex with the Inhibitor GLPG1972 | | Descriptor: | (5~{S})-5-[3-[(3~{S})-4-[3,5-bis(fluoranyl)phenyl]-3-methyl-piperazin-1-yl]-3-oxidanylidene-propyl]-5-cyclopropyl-imidazolidine-2,4-dione, A disintegrin and metalloproteinase with thrombospondin motifs 5, CALCIUM ION, ... | | Authors: | Goepfert, A, Leonard, P, Triballeau, N, Fleury, D, Mollat, P, Lamers, M. | | Deposit date: | 2020-04-03 | | Release date: | 2021-04-14 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (2.25 Å) | | Cite: | Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis.
J.Med.Chem., 64, 2021
|
|
1O4P
 | | CRYSTAL STRUCTURE OF SH2 IN COMPLEX WITH RU78791. | | Descriptor: | 2-PHENYLMALONIC ACID, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE SRC | | Authors: | Lange, G, Loenze, P, Liesum, A. | | Deposit date: | 2003-06-15 | | Release date: | 2004-02-17 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors.
J.Med.Chem., 46, 2003
|
|
1O4Q
 | | CRYSTAL STRUCTURE OF SH2 IN COMPLEX WITH RU79256. | | Descriptor: | PHENYL(SULFO)ACETIC ACID, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE SRC | | Authors: | Lange, G, Loenze, P, Liesum, A. | | Deposit date: | 2003-06-15 | | Release date: | 2004-02-17 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors.
J.Med.Chem., 46, 2003
|
|
1O4N
 | | CRYSTAL STRUCTURE OF SH2 IN COMPLEX WITH OXALIC ACID. | | Descriptor: | OXALIC ACID, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE SRC | | Authors: | Lange, G, Loenze, P, Liesum, A. | | Deposit date: | 2003-06-15 | | Release date: | 2004-02-17 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (1.6 Å) | | Cite: | Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors.
J.Med.Chem., 46, 2003
|
|
1O4J
 | | CRYSTAL STRUCTURE OF SH2 IN COMPLEX WITH ISO24. | | Descriptor: | PROTO-ONCOGENE TYROSINE-PROTEIN KINASE SRC, [(4-ETHYLPHENYL)AMINO]CARBONYLPHOSPHONIC ACID | | Authors: | Lange, G, Loenze, P, Liesum, A. | | Deposit date: | 2003-06-15 | | Release date: | 2004-02-17 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors.
J.Med.Chem., 46, 2003
|
|
1O4D
 | | CRYSTAL STRUCTURE OF SH2 IN COMPLEX WITH RU78262. | | Descriptor: | 2-FORMYLPHENYL DIHYDROGEN PHOSPHATE, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE SRC | | Authors: | Lange, G, Loenze, P, Liesum, A. | | Deposit date: | 2003-06-15 | | Release date: | 2004-02-17 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (1.85 Å) | | Cite: | Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors.
J.Med.Chem., 46, 2003
|
|
1O43
 | | CRYSTAL STRUCTURE OF SH2 IN COMPLEX WITH RU82129. | | Descriptor: | PROTO-ONCOGENE TYROSINE-PROTEIN KINASE SRC, [4-((1Z)-2-(ACETYLAMINO)-3-{[1-(1,1'-BIPHENYL-4-YLMETHYL)-2-OXOAZEPAN-3-YL]AMINO}-3-OXOPROP-1-ENYL)-2-FORMYLPHENYL]ACET IC ACID | | Authors: | Lange, G, Loenze, P, Liesum, A. | | Deposit date: | 2003-06-15 | | Release date: | 2004-02-17 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (1.5 Å) | | Cite: | Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors.
J.Med.Chem., 46, 2003
|
|
1O49
 | | CRYSTAL STRUCTURE OF SH2 IN COMPLEX WITH RU85493. | | Descriptor: | PROTO-ONCOGENE TYROSINE-PROTEIN KINASE SRC, {4-[2-ACETYLAMINO-2-(1-BIPHENYL-4-YLMETHYL-2-OXO-AZEPAN-3-YLCARBAMOYL)-ETHYL]-2-PHOSPHONO-PHENOXY}-ACETIC ACID | | Authors: | Lange, G, Loenze, P, Liesum, A. | | Deposit date: | 2003-06-15 | | Release date: | 2004-02-17 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors.
J.Med.Chem., 46, 2003
|
|
1O4G
 | | CRYSTAL STRUCTURE OF SH2 IN COMPLEX WITH DPI59. | | Descriptor: | HYDROXY(1-NAPHTHYL)METHYLPHOSPHONIC ACID, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE SRC | | Authors: | Lange, G, Loenze, P, Liesum, A. | | Deposit date: | 2003-06-15 | | Release date: | 2004-02-17 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (1.55 Å) | | Cite: | Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors.
J.Med.Chem., 46, 2003
|
|
1O4M
 | | CRYSTAL STRUCTURE OF SH2 IN COMPLEX WITH MALONICACID. | | Descriptor: | MALONIC ACID, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE SRC | | Authors: | Lange, G, Loenze, P, Liesum, A. | | Deposit date: | 2003-06-15 | | Release date: | 2004-02-17 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (1.6 Å) | | Cite: | Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors.
J.Med.Chem., 46, 2003
|
|
1O45
 | | CRYSTAL STRUCTURE OF SH2 IN COMPLEX WITH RU84687. | | Descriptor: | N-ACETYL-N-[1-(1,1'-BIPHENYL-4-YLMETHYL)-2-OXOAZEPAN-3-YL]-3-FORMYL-O-PHOSPHONOTYROSINAMIDE, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE SRC | | Authors: | Lange, G, Loenze, P, Liesum, A. | | Deposit date: | 2003-06-15 | | Release date: | 2004-02-17 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors.
J.Med.Chem., 46, 2003
|
|
1O4F
 | | CRYSTAL STRUCTURE OF SH2 IN COMPLEX WITH RU79073. | | Descriptor: | 1,2,3,4-TETRAHYDROQUINOLIN-8-YL DIHYDROGEN PHOSPHATE, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE SRC | | Authors: | Lange, G, Loenze, P, Liesum, A. | | Deposit date: | 2003-06-15 | | Release date: | 2004-02-17 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors.
J.Med.Chem., 46, 2003
|
|
1O4K
 | | CRYSTAL STRUCTURE OF SH2 IN COMPLEX WITH PASBN. | | Descriptor: | BENZYL 2-FORMYLPHENYL HYDROGEN PHOSPHATE, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE SRC | | Authors: | Lange, G, Loenze, P, Liesum, A. | | Deposit date: | 2003-06-15 | | Release date: | 2004-02-17 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (1.57 Å) | | Cite: | Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors.
J.Med.Chem., 46, 2003
|
|
4P7E
 | | Triazolopyridine compounds as selective JAK1 inhibitors: from hit identification to GLPG0634 | | Descriptor: | N-(5-{4-[(1,1-dioxidothiomorpholin-4-yl)methyl]phenyl}[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide, Tyrosine-protein kinase JAK2 | | Authors: | Menet, C.C.J, Fletcher, S, Van Lommen, G, Geney, R, Blanc, J, Smits, K, Jouannigot, N, van der Aar, E.M, Clement-Lacroix, P, Lepescheux, L, Galien, R, Vayssiere, B, Nelles, L, Christophe, T, Brys, R, Uhring, M, Ciesielski, F, Van Rompaey, L. | | Deposit date: | 2014-03-27 | | Release date: | 2014-11-19 | | Last modified: | 2023-12-20 | | Method: | X-RAY DIFFRACTION (2.4 Å) | | Cite: | Triazolopyridines as Selective JAK1 Inhibitors: From Hit Identification to GLPG0634.
J.Med.Chem., 57, 2014
|
|
1O4A
 | | CRYSTAL STRUCTURE OF SH2 IN COMPLEX WITH RU82197. | | Descriptor: | 4-[2-ACETYLAMINO-2-(1-BIPHENYL-4-YLMETHYL-2-OXO-AZEPAN-3-YLCARBAMOYL)-ETHYL]-2-FORMYL-BENZOIC ACID, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE SRC | | Authors: | Lange, G, Loenze, P, Liesum, A. | | Deposit date: | 2003-06-15 | | Release date: | 2004-02-17 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (1.5 Å) | | Cite: | Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors.
J.Med.Chem., 46, 2003
|
|
1O4B
 | | CRYSTAL STRUCTURE OF SH2 IN COMPLEX WITH RU83876. | | Descriptor: | N-ACETYL-N-[1-(1,1'-BIPHENYL-4-YLMETHYL)-2-OXOAZEPAN-3-YL]-3,4-DIPHOSPHONOPHENYLALANINAMIDE, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE SRC | | Authors: | Lange, G, Loenze, P, Liesum, A. | | Deposit date: | 2003-06-15 | | Release date: | 2004-02-17 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (1.85 Å) | | Cite: | Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors.
J.Med.Chem., 46, 2003
|
|
1O42
 | | CRYSTAL STRUCTURE OF SH2 IN COMPLEX WITH RU81843. | | Descriptor: | N-ACETYL-N-[1-(1,1'-BIPHENYL-4-YLMETHYL)-2-OXOAZEPAN-3-YL]-O-PHOSPHONOTYROSINAMIDE, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE SRC | | Authors: | Lange, G, Loenze, P, Liesum, A. | | Deposit date: | 2003-06-15 | | Release date: | 2004-02-17 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors.
J.Med.Chem., 46, 2003
|
|
1O4E
 | | CRYSTAL STRUCTURE OF SH2 IN COMPLEX WITH RU78299. | | Descriptor: | 2,6-DIFORMYL-4-METHYLPHENYL DIHYDROGEN PHOSPHATE, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE SRC | | Authors: | Lange, G, Loenze, P, Liesum, A. | | Deposit date: | 2003-06-15 | | Release date: | 2004-02-17 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors.
J.Med.Chem., 46, 2003
|
|
1O4R
 | | CRYSTAL STRUCTURE OF SH2 IN COMPLEX WITH RU78783. | | Descriptor: | (PHENYL-PHOSPHONO-METHYL)-PHOSPHONIC ACID, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE SRC | | Authors: | Lange, G, Loenze, P, Liesum, A. | | Deposit date: | 2003-06-15 | | Release date: | 2004-02-17 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (1.5 Å) | | Cite: | Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors.
J.Med.Chem., 46, 2003
|
|
1O44
 | | Crystal structure of sh2 in complex with ru85052 | | Descriptor: | 2-{4-[2-ACETYLAMINO-2-(1-BIPHENYL-4-YLMETHYL-2-OXO-AZEPAN-3-YLCARBAMOYL)-ETHYL]-2-CARBOXY-PHENYL}-MALONIC ACID, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE SRC | | Authors: | Lange, G, Loenze, P, Liesum, A. | | Deposit date: | 2003-06-15 | | Release date: | 2004-02-17 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (1.7 Å) | | Cite: | Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors.
J.Med.Chem., 46, 2003
|
|
1O4C
 | | CRYSTAL STRUCTURE OF SH2 IN COMPLEX WITH PHOSPHATE. | | Descriptor: | PHOSPHATE ION, PROTO-ONCOGENE TYROSINE-PROTEIN KINASE SRC | | Authors: | Lange, G, Loenze, P, Liesum, A. | | Deposit date: | 2003-06-15 | | Release date: | 2004-02-17 | | Last modified: | 2023-11-15 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors.
J.Med.Chem., 46, 2003
|
|
1O4I
 | | CRYSTAL STRUCTURE OF SH2 IN COMPLEX WITH PAS219. | | Descriptor: | PROTO-ONCOGENE TYROSINE-PROTEIN KINASE SRC, cyclohexylmethyl 2-formylphenyl hydrogen (S)-phosphate | | Authors: | Lange, G, Loenze, P, Liesum, A. | | Deposit date: | 2003-06-15 | | Release date: | 2004-02-17 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (1.75 Å) | | Cite: | Requirements for specific binding of low affinity inhibitor fragments to the SH2 domain of (pp60)Src are identical to those for high affinity binding of full length inhibitors.
J.Med.Chem., 46, 2003
|
|
