Reaction Details | |||
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Target | Cyclin-dependent kinase 4/G1/S-specific cyclin-D1 | ||
Ligand | BDBM50001543 | ||
Substrate/Competitor | n/a | ||
Meas. Tech. | ChEMBL_1336031 (CHEMBL3240324) | ||
IC50 | 2.0±n/a nM | ||
Citation | Li, Z; Wang, X; Eksterowicz, J; Gribble, MW; Alba, GQ; Ayres, M; Carlson, TJ; Chen, A; Chen, X; Cho, R; Connors, RV; DeGraffenreid, M; Deignan, JT; Duquette, J; Fan, P; Fisher, B; Fu, J; Huard, JN; Kaizerman, J; Keegan, KS; Li, C; Li, K; Li, Y; Liang, L; Liu, W; Lively, SE; Lo, MC; Ma, J; McMinn, DL; Mihalic, JT; Modi, K; Ngo, R; Pattabiraman, K; Piper, DE; Queva, C; Ragains, ML; Suchomel, J; Thibault, S; Walker, N; Wang, X; Wang, Z; Wanska, M; Wehn, PM; Weidner, MF; Zhang, AJ; Zhao, X; Kamb, A; Wickramasinghe, D; Dai, K; McGee, LR; Medina, JC Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3. J Med Chem57:3430-49 (2014) [PubMed] Article | ||
More Info.: | Get all data from this article, Assay Method | ||
Cyclin-dependent kinase 4/G1/S-specific cyclin-D1 | |||
Name: | Cyclin-dependent kinase 4/G1/S-specific cyclin-D1 | ||
Synonyms: | CDK4/CycD | CDK4/CycD1 | CDK4/Cyclin D1 | CDK4/D1 | Cyclin-Dependent Kinase 4 (CDK4) | Cyclin-dependent kinase 4 | Cyclin-dependent kinase 4/G1/S-specific cyclin D1 | Cyclin-dependent kinase 4/cyclin D1 | ||
Type: | Protein Complex | ||
Mol. Mass.: | n/a | ||
Description: | CDK4/D1 complexes were purified from insect cells co-infected with baculovirus vectors containing each of the components. | ||
Components: | This complex has 2 components. | ||
Component 1 | |||
Name: | Cyclin-dependent kinase 4 | ||
Synonyms: | CDK4 | CDK4_HUMAN | Cell division protein kinase 4 | Cyclin-dependent kinase 4 (CDK 4) | PSK-J3 | ||
Type: | Enzyme Subunit | ||
Mol. Mass.: | 33731.96 | ||
Organism: | Homo sapiens (Human) | ||
Description: | P11802 | ||
Residue: | 303 | ||
Sequence: |
| ||
Component 2 | |||
Name: | G1/S-specific cyclin-D1 | ||
Synonyms: | B-cell lymphoma 1 protein | BCL-1 | BCL-1 oncogene | BCL1 | CCND1 | CCND1_HUMAN | PRAD1 | PRAD1 oncogene | ||
Type: | Enzyme Subunit | ||
Mol. Mass.: | 33717.70 | ||
Organism: | Homo sapiens (Human) | ||
Description: | n/a | ||
Residue: | 295 | ||
Sequence: |
| ||
BDBM50001543 | |||
n/a | |||
Name | BDBM50001543 | ||
Synonyms: | CHEMBL3237708 | ||
Type | Small organic molecule | ||
Emp. Form. | C26H32N8 | ||
Mol. Mass. | 456.5859 | ||
SMILES | C[C@H]1CC[C@@H](CC1)n1c2cnccc2c2cnc(Nc3ccc(cn3)N3CCC(N)CC3)nc12 |r,wU:4.7,wD:1.0,(11.29,-49.99,;10.82,-48.52,;11.85,-47.38,;11.38,-45.91,;9.88,-45.59,;8.84,-46.74,;9.31,-48.2,;9.41,-44.13,;10.31,-42.88,;11.84,-42.73,;12.48,-41.32,;11.56,-40.07,;10.04,-40.23,;9.41,-41.63,;7.94,-42.1,;6.6,-41.34,;5.27,-42.12,;5.28,-43.65,;3.95,-44.42,;3.96,-45.96,;5.29,-46.72,;5.3,-48.25,;3.96,-49.03,;2.63,-48.27,;2.62,-46.73,;3.97,-50.58,;2.64,-51.35,;2.64,-52.89,;3.98,-53.66,;3.98,-55.2,;5.31,-52.88,;5.31,-51.34,;6.62,-44.42,;7.94,-43.65,)| | ||
Structure |