| Reaction Details |
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 | Report a problem with these data |
| Target | Cyclin-dependent kinase 2/G1/S-specific cyclin-E1 |
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| Ligand | BDBM12612 |
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| Substrate/Competitor | GST-Rb fusion protein |
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| Meas. Tech. | Homogeneous Time-resolved Fluorescence (HTRF) Assay |
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| Ki | 51±n/a nM |
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| Citation |  Chu, XJ; DePinto, W; Bartkovitz, D; So, SS; Vu, BT; Packman, K; Lukacs, C; Ding, Q; Jiang, N; Wang, K; Goelzer, P; Yin, X; Smith, MA; Higgins, BX; Chen, Y; Xiang, Q; Moliterni, J; Kaplan, G; Graves, B; Lovey, A; Fotouhi, 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 |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| Cyclin-dependent kinase 2/G1/S-specific cyclin-E1 |
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| Name: | Cyclin-dependent kinase 2/G1/S-specific cyclin-E1 |
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| Synonyms: | CDK2/CycE | CDK2/Cyclin E | CDK2/E | CDK2/E1 | Cyclin-Dependent Kinase 2 (CDK2) | Cyclin-dependent kinase 2/G1/S-specific cyclin E1 | Cyclin-dependent kinase 2/cyclin E1 |
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| Type: | Protein |
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| Mol. Mass.: | n/a |
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| Description: | n/a |
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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: | G1/S-specific cyclin-E1 |
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| Synonyms: | CCNE | CCNE1 | CCNE1_HUMAN |
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| Type: | Enzyme Subunit |
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| Mol. Mass.: | 47073.17 |
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| Organism: | Homo sapiens (Human) |
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| Description: | n/a |
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| Residue: | 410 |
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| Sequence: | MPRERRERDAKERDTMKEDGGAEFSARSRKRKANVTVFLQDPDEEMAKIDRTARDQCGSQ
PWDNNAVCADPCSLIPTPDKEDDDRVYPNSTCKPRIIAPSRGSPLPVLSWANREEVWKIM
LNKEKTYLRDQHFLEQHPLLQPKMRAILLDWLMEVCEVYKLHRETFYLAQDFFDRYMATQ
ENVVKTLLQLIGISSLFIAAKLEEIYPPKLHQFAYVTDGACSGDEILTMELMIMKALKWR
LSPLTIVSWLNVYMQVAYLNDLHEVLLPQYPQQIFIQIAELLDLCVLDVDCLEFPYGILA
ASALYHFSSSELMQKVSGYQWCDIENCVKWMVPFAMVIRETGSSKLKHFRGVADEDAHNI
QTHRDSLDLLDKARAKKAMLSEQNRASPLPSGLLTPPQSGKKQSSGPEMA
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| BDBM12612 |
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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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