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Target
Cyclin-dependent kinase 4/G1/S-specific cyclin-D1
Ligand
BDBM50001582
Substrate
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 Chem 57:3430-49 (2014) [PubMed] Article
More Info.:
Target
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:
MATSRYEPVAEIGVGAYGTVYKARDPHSGHFVALKSVRVPNGGGGGGGLPISTVREVALLRRLEAFEHPNVVRLMDVCATSRTDREIKVTLVFEHVDQDLRTYLDKAPPPGLPAETIKDLMRQFLRGLDFLHANCIVHRDLKPENILVTSGGTVKLADFGLARIYSYQMALTPVVVTLWYRAPEVLLQSTYATPVDMWSVGCIFAEMFRRKPLFCGNSEADQLGKIFDLIGLPPEDDWPRDVSLPRGAFPPRGPRPVQSVVPEMEESGAQLLLEMLTFNPHKRISAFRALQHSYLHKDEGNPE
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:
MEHQLLCCEVETIRRAYPDANLLNDRVLRAMLKAEETCAPSVSYFKCVQKEVLPSMRKIVATWMLEVCEEQKCEEEVFPLAMNYLDRFLSLEPVKKSRLQLLGATCMFVASKMKETIPLTAEKLCIYTDNSIRPEELLQMELLLVNKLKWNLAAMTPHDFIEHFLSKMPEAEENKQIIRKHAQTFVALCATDVKFISNPPSMVAAGSVVAAVQGLNLRSPNNFLSYYRLTRFLSRVIKCDPDCLRACQEQIEALLESSLRQAQQNMDPKAAEEEEEEEEEVDLACTPTDVRDVDI
Inhibitor
Name:
BDBM50001582
Synonyms:
CHEMBL3237717
Type:
Small organic molecule
Emp. Form.:
C29H34N8O
Mol. Mass.:
510.6333
SMILES:
C[C@H]1CC[C@@H](CC1)n1c2cnccc2c2cnc(Nc3ccc(cn3)N3CCC4(CCC(=O)N4)CC3)nc12 |r,wU:4.7,wD:1.0,(34.23,-57.43,;33.76,-55.97,;34.8,-54.83,;34.33,-53.35,;32.82,-53.04,;31.79,-54.18,;32.26,-55.64,;32.35,-51.57,;33.26,-50.32,;34.79,-50.17,;35.42,-48.76,;34.51,-47.51,;32.98,-47.67,;32.36,-49.07,;30.88,-49.55,;29.54,-48.78,;28.21,-49.56,;28.23,-51.09,;26.89,-51.86,;26.88,-53.4,;28.19,-54.17,;28.18,-55.7,;26.84,-56.46,;25.52,-55.68,;25.54,-54.15,;26.83,-57.99,;25.49,-58.74,;25.47,-60.28,;26.8,-61.07,;25.55,-61.97,;26.03,-63.44,;27.57,-63.44,;28.47,-64.69,;28.04,-61.97,;28.14,-60.31,;28.16,-58.77,;29.56,-51.86,;30.88,-51.09,)|