| Reaction Details |
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 | Report a problem with these data |
| Target | Cyclin-A2/Cyclin-dependent kinase 2 |
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| Ligand | BDBM6274 |
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| Substrate/Competitor | GST-Rb fusion protein |
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| Meas. Tech. | CDKs Assay |
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| IC50 | 58±n/a nM |
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| Citation |  Barvian, M; Boschelli, DH; Cossrow, J; Dobrusin, E; Fattaey, A; Fritsch, A; Fry, D; Harvey, P; Keller, P; Garrett, M; La, F; Leopold, W; McNamara, D; Quin, M; Trumpp-Kallmeyer, S; Toogood, P; Wu, Z; Zhang, E Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. J Med Chem43:4606-16 (2000) [PubMed] Article |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| Cyclin-A2/Cyclin-dependent kinase 2 |
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| Name: | Cyclin-A2/Cyclin-dependent kinase 2 |
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| Synonyms: | CDK2-CyclinA | CDK2/A | CDK2/Cyclin A | CDK2/Cyclin A2 | Cyclin A2/dependent kinase 2 | Cyclin-Dependent Kinase 2 (CDK2) | Cyclin-Dependent Kinase 2 (CDK2A) |
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| Type: | Protein Complex |
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| Mol. Mass.: | n/a |
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| Description: | Cdk2/Cyclin A kinase was purified from insect cells coinfected with Cyclin A/Cdk2 baculovirus. |
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| Components: | This complex has 2 components. |
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| Component 1 |
| Name: | Cyclin-dependent kinase 2 |
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| Synonyms: | CDK2 | CDK2-Kinase | CDK2_HUMAN | CDKN2 | Cell division protein kinase 2 | Cyclin-dependent kinase 2 (CDK2) | Protein cereblon/Cyclin-dependent kinase 2 | p33 protein kinase |
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| Type: | Enzyme Subunit |
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| Mol. Mass.: | 33938.17 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P24941 |
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| Residue: | 298 |
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| Sequence: | MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNH
PNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHS
HRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYY
STAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSF
PKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
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| Component 2 |
| Name: | Cyclin-A2 |
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| Synonyms: | CCN1 | CCNA | CCNA1 | CCNA2 | CCNA2_HUMAN | Cyclin A | Cyclin-A |
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| Type: | Enzyme Subunit |
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| Mol. Mass.: | 48550.19 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P20248 |
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| Residue: | 432 |
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| Sequence: | MLGNSAPGPATREAGSALLALQQTALQEDQENINPEKAAPVQQPRTRAALAVLKSGNPRG
LAQQQRPKTRRVAPLKDLPVNDEHVTVPPWKANSKQPAFTIHVDEAEKEAQKKPAESQKI
EREDALAFNSAISLPGPRKPLVPLDYPMDGSFESPHTMDMSIILEDEKPVSVNEVPDYHE
DIHTYLREMEVKCKPKVGYMKKQPDITNSMRAILVDWLVEVGEEYKLQNETLHLAVNYID
RFLSSMSVLRGKLQLVGTAAMLLASKFEEIYPPEVAEFVYITDDTYTKKQVLRMEHLVLK
VLTFDLAAPTVNQFLTQYFLHQQPANCKVESLAMFLGELSLIDADPYLKYLPSVIAGAAF
HLALYTVTGQSWPESLIRKTGYTLESLKPCLMDLHQTYLKAPQHAQQSIREKYKNSKYHG
VSLLNPPETLNL
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| BDBM6274 |
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| GST-Rb fusion protein |
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| Name: | GST-Rb fusion protein |
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| Synonyms: | Glutathione S-transferase (GST)-retinoblastoma (Rb) fusion | Histidine-tagged retinoblastoma protein | RB1 | RB_HUMAN | Rb | retinoblastoma |
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| Type: | Other Protein Type |
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| Mol. Mass.: | 106410.17 |
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| Organism: | Homo sapiens (Human) |
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| Description: | GST-60 kDa Rb fusion protein (comprising amino acids 378 to 928 of retinoblastoma) |
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| Residue: | 928 |
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| Sequence: | MPPKTPRKTAATAAAAAAEPPAPPPPPPPEEDPEQDSGPEDLPLVRLEFEETEEPDFTAL
CQKLKIPDHVRERAWLTWEKVSSVDGVLGGYIQKKKELWGICIFIARVDLDEMSFTLLSY
RKTYEISVHKFFNLLKEIDTSTKVDNAMSRLLKKYDVLFALFSKLERTCELIYLTQPSSS
ISTEINSALVLKVSWITFLLAKGEVLQMEDDLVISFQLMLCVLDYFIKLSPPMLLKEPYK
TAVIPINGSPRTPRRGQNRSARIAKQLENDTRIIEVLCKEHECNIDEVKNVYFKNFIPFM
NSLGLVTSNGLPEVENLSKRYEEIYLKNKDLDRRLFLDHDKTLQTDSIDSFETQRTPRKS
NLDEEVNIIPPHTPVRTVMNTIQQLMMILNSASDQPSENLISYFNNCTVNPKESILKRVK
DIGYIFKEKFAKAVGQGCVEIGSQRYKLGVRLYYRVMESMLKSEEERLSIQNFSKLLNDN
IFHMSLLACALEVVMATYSRSTSQNLDSGTDLSFPWILNVLNLKAFDFYKVIESFIKAEG
NLTREMIKHLERCEHRIMESLAWLSDSPLFDLIKQSKDREGPTDHLESACPLNLPLQNNH
TAADMYLSPVRSPKKKGSTTRVNSTANAETQATSAFQTQKPLKSTSLSLFYKKVYRLAYL
RLNTLCERLLSEHPELEHIIWTLFQHTLQNEYELMRDRHLDQIMMCSMYGICKVKNIDLK
FKIIVTAYKDLPHAVQETFKRVLIKEEEYDSIIVFYNSVFMQRLKTNILQYASTRPPTLS
PIPHIPRSPYKFPSSPLRIPGGNIYISPLKSPYKISEGLPTPTKMTPRSRILVSIGESFG
TSEKFQKINQMVCNSDRVLKRSAEGSNPPKPLKKLRFDIEGSDEADGSKHLPGESKFQQK
LAEMTSTRTRMQKQKMNDSMDTSNKEEK
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