Reaction Details | |||
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Target | Cyclin-dependent kinase 4/G1/S-specific cyclin-D1 | ||
Ligand | BDBM112464 | ||
Substrate/Competitor | n/a | ||
Meas. Tech. | ChEMBL_1336031 (CHEMBL3240324) | ||
IC50 | 3.0±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: |
| ||
BDBM112464 | |||
n/a | |||
Name | BDBM112464 | ||
Synonyms: | US8623885, 5 | ||
Type | Small organic molecule | ||
Emp. Form. | C26H29N7O2 | ||
Mol. Mass. | 471.5542 | ||
SMILES | C[C@H]1CC[C@@H](CC1)n1c2cnccc2c2cnc(Nc3ccc4CN(CCc4n3)C(=O)CO)nc12 |r,wU:4.7,wD:1.0,(4.13,-3.21,;3.73,-1.73,;4.82,-.64,;4.42,.85,;2.93,1.25,;1.84,.16,;2.24,-1.33,;2.53,2.74,;3.44,3.98,;4.97,4.14,;5.6,5.55,;4.69,6.8,;3.16,6.64,;2.53,5.23,;1.07,4.75,;-.26,5.52,;-1.6,4.75,;-1.6,3.21,;-2.93,2.44,;-2.93,.9,;-1.6,.13,;-1.6,-1.41,;-2.93,-2.18,;-2.93,-3.72,;-4.26,-4.49,;-5.6,-3.72,;-5.6,-2.18,;-4.26,-1.41,;-4.26,.13,;-4.26,-6.03,;-5.6,-6.8,;-2.93,-6.8,;-1.6,-6.03,;-.26,2.44,;1.07,3.21,)| | ||
Structure |