Reaction Details |
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Target | Cyclin-dependent kinase 4/G1/S-specific cyclin-D1 |
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Ligand | BDBM6867 |
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Substrate/Competitor | GST-Rb fusion protein |
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Meas. Tech. | Kinase Inhibition Assay |
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IC50 | 190±n/a nM |
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Citation | Lin, R; Connolly, PJ; Huang, S; Wetter, SK; Lu, Y; Murray, WV; Emanuel, SL; Gruninger, RH; Fuentes-Pesquera, AR; Rugg, CA; Middleton, SA; Jolliffe, LK 1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities. J Med Chem48:4208-11 (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 |
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Name: | Cyclin-dependent kinase 4/G1/S-specific cyclin-D1 |
Synonyms: | CDK4/Cyclin D1 | Cyclin-Dependent Kinase 4 (CDK4) |
Type: | Protein Complex |
Mol. Mass.: | n/a |
Description: | The recombinant CDK4/D1 complex was made by co-infecting insect cells with viruses carrying CDK4 and Cyclin D1. |
Components: | This complex has 2 components. |
Component 1 |
Name: | G1/S-specific cyclin-D1 |
Synonyms: | CCND1_MOUSE | Ccnd1 | Cyclin D1 | Cyl-1 |
Type: | Enzyme Subunit |
Mol. Mass.: | 33418.84 |
Organism: | Mus musculus (mouse) |
Description: | n/a |
Residue: | 295 |
Sequence: | MEHQLLCCEVETIRRAYPDTNLLNDRVLRAMLKTEETCAPSVSYFKCVQKEIVPSMRKIV
ATWMLEVCEEQKCEEEVFPLAMNYLDRFLSLEPLKKSRLQLLGATCMFVASKMKETIPLT
AEKLCIYTDNSIRPEELLQMELLLVNKLKWNLAAMTPHDFIEHFLSKMPEADENKQTIRK
HAQTFVALCATDVKFISNPPSMVAAGSVVAAMQGLNLGSPNNFLSCYRTTHFLSRVIKCD
PDCLRACQEQIEALLESSLRQAQQNVDPKATEEEGEVEEEAGLACTPTDVRDVDI
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Component 2 |
Name: | Cyclin-dependent kinase 4 |
Synonyms: | CDK4_MOUSE | Cdk4 | Crk3 | cyclin-dependent kinase 4 |
Type: | Enzyme Subunit |
Mol. Mass.: | 33750.96 |
Organism: | Mus musculus (mouse) |
Description: | n/a |
Residue: | 303 |
Sequence: | MAATRYEPVAEIGVGAYGTVYKARDPHSGHFVALKSVRVPNGGAAGGGLPVSTVREVALL
RRLEAFEHPNVVRLMDVCATSRTDRDIKVTLVFEHIDQDLRTYLDKAPPPGLPVETIKDL
MRQFLSGLDFLHANCIVHRDLKPENILVTSNGTVKLADFGLARIYSYQMALTPVVVTLWY
RAPEVLLQSTYATPVDMWSVGCIFAEMFRRKPLFCGNSEADQLGKIFDLIGLPPEDDWPR
EVSLPRGAFAPRGPRPVQSVVPEMEESGAQLLLEMLTFNPHKRISAFRALQHSYLHKEES
DAE
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BDBM6867 |
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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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