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TargetCyclin-Dependent Kinase 4 (CDK4)
LigandBDBM12611
Substrate/CompetitorGST-Rb fusion protein
Meas. Tech.Homogeneous Time-resolved Fluorescence (HTRF) Assay
Ki 14±n/a nM
Citation Chu, XJDePinto, WBartkovitz, DSo, SSVu, BTPackman, KLukacs, CDing, QJiang, NWang, KGoelzer, PYin, XSmith, MAHiggins, BXChen, YXiang, QMoliterni, JKaplan, GGraves, BLovey, AFotouhi, N Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity. J Med Chem49:6549-60 (2006) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Cyclin-Dependent Kinase 4 (CDK4)
Name:Cyclin-Dependent Kinase 4 (CDK4)
Synonyms:CDK4/CycD | CDK4/CycD1 | CDK4/Cyclin D1 | CDK4/D1 | 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:CDK4/CDK9
Synonyms:CDK4 | 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 | CCND1 | 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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BDBM12611
NameBDBM12611
Synonyms:2,4-Diamino-5-ketopyrimidine 29 | 2-N-(1-methanesulfonylpiperidin-4-yl)-5-[(2-methoxyphenyl)carbonyl]pyrimidine-2,4-diamine | [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2-methoxyphenyl)methanone
TypeSmall organic molecule
Emp. Form.C18H23N5O4S
Mol. Mass.405.471
SMILESCOc1ccccc1C(=O)c1cnc(NC2CCN(CC2)S(C)(=O)=O)nc1N
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
GST-Rb fusion protein
Name:GST-Rb fusion protein
Synonyms:Glutathione S-transferase (GST)-retinoblastoma (Rb) fusion | Histidine-tagged retinoblastoma protein | Rb | retinoblastoma
Type:Other Protein Type
Mol. Mass.:106410.17
Organism:Homo sapiens (Human)
Description:GST-60 kDa Rb fusion protein (comprising amino acids 378 to 928 of retinoblastoma)
Residue:928
Sequence:
MPPKTPRKTAATAAAAAAEPPAPPPPPPPEEDPEQDSGPEDLPLVRLEFEETEEPDFTAL
CQKLKIPDHVRERAWLTWEKVSSVDGVLGGYIQKKKELWGICIFIARVDLDEMSFTLLSY
RKTYEISVHKFFNLLKEIDTSTKVDNAMSRLLKKYDVLFALFSKLERTCELIYLTQPSSS
ISTEINSALVLKVSWITFLLAKGEVLQMEDDLVISFQLMLCVLDYFIKLSPPMLLKEPYK
TAVIPINGSPRTPRRGQNRSARIAKQLENDTRIIEVLCKEHECNIDEVKNVYFKNFIPFM
NSLGLVTSNGLPEVENLSKRYEEIYLKNKDLDRRLFLDHDKTLQTDSIDSFETQRTPRKS
NLDEEVNIIPPHTPVRTVMNTIQQLMMILNSASDQPSENLISYFNNCTVNPKESILKRVK
DIGYIFKEKFAKAVGQGCVEIGSQRYKLGVRLYYRVMESMLKSEEERLSIQNFSKLLNDN
IFHMSLLACALEVVMATYSRSTSQNLDSGTDLSFPWILNVLNLKAFDFYKVIESFIKAEG
NLTREMIKHLERCEHRIMESLAWLSDSPLFDLIKQSKDREGPTDHLESACPLNLPLQNNH
TAADMYLSPVRSPKKKGSTTRVNSTANAETQATSAFQTQKPLKSTSLSLFYKKVYRLAYL
RLNTLCERLLSEHPELEHIIWTLFQHTLQNEYELMRDRHLDQIMMCSMYGICKVKNIDLK
FKIIVTAYKDLPHAVQETFKRVLIKEEEYDSIIVFYNSVFMQRLKTNILQYASTRPPTLS
PIPHIPRSPYKFPSSPLRIPGGNIYISPLKSPYKISEGLPTPTKMTPRSRILVSIGESFG
TSEKFQKINQMVCNSDRVLKRSAEGSNPPKPLKKLRFDIEGSDEADGSKHLPGESKFQQK
LAEMTSTRTRMQKQKMNDSMDTSNKEEK
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