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TargetCyclin-dependent kinase 4/G1/S-specific cyclin-D1
LigandBDBM112464
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1336031 (CHEMBL3240324)
IC50 3.0±n/a nM
Citation Li, ZWang, XEksterowicz, JGribble, MWAlba, GQAyres, MCarlson, TJChen, AChen, XCho, RConnors, RVDeGraffenreid, MDeignan, JTDuquette, JFan, PFisher, BFu, JHuard, JNKaizerman, JKeegan, KSLi, CLi, KLi, YLiang, LLiu, WLively, SELo, MCMa, JMcMinn, DLMihalic, JTModi, KNgo, RPattabiraman, KPiper, DEQueva, CRagains, MLSuchomel, JThibault, SWalker, NWang, XWang, ZWanska, MWehn, PMWeidner, MFZhang, AJZhao, XKamb, AWickramasinghe, DDai, KMcGee, LRMedina, 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
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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:
MATSRYEPVAEIGVGAYGTVYKARDPHSGHFVALKSVRVPNGGGGGGGLPISTVREVALL
RRLEAFEHPNVVRLMDVCATSRTDREIKVTLVFEHVDQDLRTYLDKAPPPGLPAETIKDL
MRQFLRGLDFLHANCIVHRDLKPENILVTSGGTVKLADFGLARIYSYQMALTPVVVTLWY
RAPEVLLQSTYATPVDMWSVGCIFAEMFRRKPLFCGNSEADQLGKIFDLIGLPPEDDWPR
DVSLPRGAFPPRGPRPVQSVVPEMEESGAQLLLEMLTFNPHKRISAFRALQHSYLHKDEG
NPE
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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:
MEHQLLCCEVETIRRAYPDANLLNDRVLRAMLKAEETCAPSVSYFKCVQKEVLPSMRKIV
ATWMLEVCEEQKCEEEVFPLAMNYLDRFLSLEPVKKSRLQLLGATCMFVASKMKETIPLT
AEKLCIYTDNSIRPEELLQMELLLVNKLKWNLAAMTPHDFIEHFLSKMPEAEENKQIIRK
HAQTFVALCATDVKFISNPPSMVAAGSVVAAVQGLNLRSPNNFLSYYRLTRFLSRVIKCD
PDCLRACQEQIEALLESSLRQAQQNMDPKAAEEEEEEEEEVDLACTPTDVRDVDI
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BDBM112464
n/a
NameBDBM112464
Synonyms:US8623885, 5
TypeSmall organic molecule
Emp. Form.C26H29N7O2
Mol. Mass.471.5542
SMILESC[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
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