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Target
Cyclin-dependent kinase 4/G1/S-specific cyclin-D1 [L188C]
Ligand
BDBM6383
Substrate
GST-Rb fusion protein
Meas. Tech.
CDKs Assay
IC50
5±n/a nM
Citation
VanderWel, SN; Harvey, PJ; McNamara, DJ; Repine, JT; Keller, PR; Quin, J; Booth, RJ; Elliott, WL; Dobrusin, EM; Fry, DW; Toogood, PL Pyrido[2,3-d]pyrimidin-7-ones as specific inhibitors of cyclin-dependent kinase 4. J Med Chem 48:2371-87 (2005) [PubMed] Article
More Info.:
Target
Name:
Cyclin-dependent kinase 4/G1/S-specific cyclin-D1 [L188C]
Synonyms:
CDK4/Cyclin D | Cyclin-Dependent Kinase 4 (CDK4)
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
CDK4/D 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 [L188C]
Synonyms:
BCL1 | CCND1 | CCND1_HUMAN | Cyclin D | PRAD1
Type:
Enzyme Subunit
Mol. Mass.:
33634.57
Organism:
Homo sapiens (Human)
Description:
P24385[L188C]
Residue:
295
Sequence:
MEHQLLCCEVETIRRAYPDANLLNDRVLRAMLKAEETCAPSVSYFKCVQKEVLPSMRKIVATWMLEVCEEQKCEEEVFPLAMNYLDRFLSLEPVKKSRLQLLGATCMFVASKMKETIPLTAEKLCIYTDGSIRPEELLQMELLLVNKLKWNLAAMTPHDFIEHFLSKMPEAEENKQIIRKHAQTFVASCATDVKFISNPPSMVAAGSVVAAVQGLNLRSPNNFLSYYRLTRFLSRVIKCDPDCLRACQEQIEALLESSLRQAQQNMDPKAAEEEEEEEEEVDLACTPTDVRDVDI
Inhibitor
Name:
BDBM6383
Synonyms:
8-Cyclopentyl-6-iodo-5-methyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one | 8-cyclopentyl-6-iodo-5-methyl-2-{[4-(piperazin-1-yl)phenyl]amino}-7H,8H-pyrido[2,3-d]pyrimidin-7-one | pyrido[2,3-d]pyrimidin-7-one 30
Type:
Small organic molecule
Emp. Form.:
C23H27IN6O
Mol. Mass.:
530.4046
SMILES:
Cc1c(I)c(=O)n(C2CCCC2)c2nc(Nc3ccc(cc3)N3CCNCC3)ncc12
Substrate
Name:
GST-Rb fusion protein
Synonyms:
Glutathione S-transferase (GST)-retinoblastoma (Rb) fusion | Histidine-tagged retinoblastoma protein | RB1 | RB_HUMAN | 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:
MPPKTPRKTAATAAAAAAEPPAPPPPPPPEEDPEQDSGPEDLPLVRLEFEETEEPDFTALCQKLKIPDHVRERAWLTWEKVSSVDGVLGGYIQKKKELWGICIFIARVDLDEMSFTLLSYRKTYEISVHKFFNLLKEIDTSTKVDNAMSRLLKKYDVLFALFSKLERTCELIYLTQPSSSISTEINSALVLKVSWITFLLAKGEVLQMEDDLVISFQLMLCVLDYFIKLSPPMLLKEPYKTAVIPINGSPRTPRRGQNRSARIAKQLENDTRIIEVLCKEHECNIDEVKNVYFKNFIPFMNSLGLVTSNGLPEVENLSKRYEEIYLKNKDLDRRLFLDHDKTLQTDSIDSFETQRTPRKSNLDEEVNIIPPHTPVRTVMNTIQQLMMILNSASDQPSENLISYFNNCTVNPKESILKRVKDIGYIFKEKFAKAVGQGCVEIGSQRYKLGVRLYYRVMESMLKSEEERLSIQNFSKLLNDNIFHMSLLACALEVVMATYSRSTSQNLDSGTDLSFPWILNVLNLKAFDFYKVIESFIKAEGNLTREMIKHLERCEHRIMESLAWLSDSPLFDLIKQSKDREGPTDHLESACPLNLPLQNNHTAADMYLSPVRSPKKKGSTTRVNSTANAETQATSAFQTQKPLKSTSLSLFYKKVYRLAYLRLNTLCERLLSEHPELEHIIWTLFQHTLQNEYELMRDRHLDQIMMCSMYGICKVKNIDLKFKIIVTAYKDLPHAVQETFKRVLIKEEEYDSIIVFYNSVFMQRLKTNILQYASTRPPTLSPIPHIPRSPYKFPSSPLRIPGGNIYISPLKSPYKISEGLPTPTKMTPRSRILVSIGESFGTSEKFQKINQMVCNSDRVLKRSAEGSNPPKPLKKLRFDIEGSDEADGSKHLPGESKFQQKLAEMTSTRTRMQKQKMNDSMDTSNKEEK