Reaction Details |
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Target | Cyclin-dependent kinase 4/G1/S-specific cyclin-D1 [L188C] |
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Ligand | BDBM6376 |
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Substrate/Competitor | GST-Rb fusion protein |
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Meas. Tech. | CDKs Assay |
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IC50 | 65±n/a nM |
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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 Chem48:2371-87 (2005) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Cyclin-dependent kinase 4/G1/S-specific cyclin-D1 [L188C] |
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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: | MATSRYEPVAEIGVGAYGTVYKARDPHSGHFVALKSVRVPNGGGGGGGLPISTVREVALL
RRLEAFEHPNVVRLMDVCATSRTDREIKVTLVFEHVDQDLRTYLDKAPPPGLPAETIKDL
MRQFLRGLDFLHANCIVHRDLKPENILVTSGGTVKLADFGLARIYSYQMALTPVVVTLWY
RAPEVLLQSTYATPVDMWSVGCIFAEMFRRKPLFCGNSEADQLGKIFDLIGLPPEDDWPR
DVSLPRGAFPPRGPRPVQSVVPEMEESGAQLLLEMLTFNPHKRISAFRALQHSYLHKDEG
NPE
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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: | MEHQLLCCEVETIRRAYPDANLLNDRVLRAMLKAEETCAPSVSYFKCVQKEVLPSMRKIV
ATWMLEVCEEQKCEEEVFPLAMNYLDRFLSLEPVKKSRLQLLGATCMFVASKMKETIPLT
AEKLCIYTDGSIRPEELLQMELLLVNKLKWNLAAMTPHDFIEHFLSKMPEAEENKQIIRK
HAQTFVASCATDVKFISNPPSMVAAGSVVAAVQGLNLRSPNNFLSYYRLTRFLSRVIKCD
PDCLRACQEQIEALLESSLRQAQQNMDPKAAEEEEEEEEEVDLACTPTDVRDVDI
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BDBM6376 |
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GST-Rb fusion protein |
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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: | MPPKTPRKTAATAAAAAAEPPAPPPPPPPEEDPEQDSGPEDLPLVRLEFEETEEPDFTAL
CQKLKIPDHVRERAWLTWEKVSSVDGVLGGYIQKKKELWGICIFIARVDLDEMSFTLLSY
RKTYEISVHKFFNLLKEIDTSTKVDNAMSRLLKKYDVLFALFSKLERTCELIYLTQPSSS
ISTEINSALVLKVSWITFLLAKGEVLQMEDDLVISFQLMLCVLDYFIKLSPPMLLKEPYK
TAVIPINGSPRTPRRGQNRSARIAKQLENDTRIIEVLCKEHECNIDEVKNVYFKNFIPFM
NSLGLVTSNGLPEVENLSKRYEEIYLKNKDLDRRLFLDHDKTLQTDSIDSFETQRTPRKS
NLDEEVNIIPPHTPVRTVMNTIQQLMMILNSASDQPSENLISYFNNCTVNPKESILKRVK
DIGYIFKEKFAKAVGQGCVEIGSQRYKLGVRLYYRVMESMLKSEEERLSIQNFSKLLNDN
IFHMSLLACALEVVMATYSRSTSQNLDSGTDLSFPWILNVLNLKAFDFYKVIESFIKAEG
NLTREMIKHLERCEHRIMESLAWLSDSPLFDLIKQSKDREGPTDHLESACPLNLPLQNNH
TAADMYLSPVRSPKKKGSTTRVNSTANAETQATSAFQTQKPLKSTSLSLFYKKVYRLAYL
RLNTLCERLLSEHPELEHIIWTLFQHTLQNEYELMRDRHLDQIMMCSMYGICKVKNIDLK
FKIIVTAYKDLPHAVQETFKRVLIKEEEYDSIIVFYNSVFMQRLKTNILQYASTRPPTLS
PIPHIPRSPYKFPSSPLRIPGGNIYISPLKSPYKISEGLPTPTKMTPRSRILVSIGESFG
TSEKFQKINQMVCNSDRVLKRSAEGSNPPKPLKKLRFDIEGSDEADGSKHLPGESKFQQK
LAEMTSTRTRMQKQKMNDSMDTSNKEEK
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