Reaction Details |
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Target | Cyclin-dependent kinase 2/G1/S-specific cyclin-E1 |
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Ligand | BDBM6860 |
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Substrate/Competitor | Rb(21) |
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Meas. Tech. | Kinase Inhibition Assay |
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pH | 7±n/a |
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Temperature | 295.15±n/a K |
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IC50 | 520±n/a nM |
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Citation | Zhu, G; Conner, SE; Zhou, X; Shih, C; Li, T; Anderson, BD; Brooks, HB; Campbell, RM; Considine, E; Dempsey, JA; Faul, MM; Ogg, C; Patel, B; Schultz, RM; Spencer, CD; Teicher, B; Watkins, SA Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors. J Med Chem46:2027-30 (2003) [PubMed] Article |
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More Info.: | Get all data from this article, Inhibition_Run data, 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 |
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 |
Type: | Protein |
Mol. Mass.: | n/a |
Description: | n/a |
Components: | This complex has 2 components. |
Component 1 |
Name: | Cyclin-dependent kinase 2 |
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 |
Type: | Enzyme Subunit |
Mol. Mass.: | 33938.17 |
Organism: | Homo sapiens (Human) |
Description: | P24941 |
Residue: | 298 |
Sequence: | MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNH
PNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHS
HRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYY
STAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSF
PKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
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Component 2 |
Name: | G1/S-specific cyclin-E1 |
Synonyms: | CCNE | CCNE1 | CCNE1_HUMAN |
Type: | Enzyme Subunit |
Mol. Mass.: | 47073.17 |
Organism: | Homo sapiens (Human) |
Description: | n/a |
Residue: | 410 |
Sequence: | MPRERRERDAKERDTMKEDGGAEFSARSRKRKANVTVFLQDPDEEMAKIDRTARDQCGSQ
PWDNNAVCADPCSLIPTPDKEDDDRVYPNSTCKPRIIAPSRGSPLPVLSWANREEVWKIM
LNKEKTYLRDQHFLEQHPLLQPKMRAILLDWLMEVCEVYKLHRETFYLAQDFFDRYMATQ
ENVVKTLLQLIGISSLFIAAKLEEIYPPKLHQFAYVTDGACSGDEILTMELMIMKALKWR
LSPLTIVSWLNVYMQVAYLNDLHEVLLPQYPQQIFIQIAELLDLCVLDVDCLEFPYGILA
ASALYHFSSSELMQKVSGYQWCDIENCVKWMVPFAMVIRETGSSKLKHFRGVADEDAHNI
QTHRDSLDLLDKARAKKAMLSEQNRASPLPSGLLTPPQSGKKQSSGPEMA
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BDBM6860 |
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Rb(21) |
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Name: | Rb(21) |
Synonyms: | C-terminal retinoblastoma protein | RB1 | RB_HUMAN |
Type: | Other Protein Type |
Mol. Mass.: | 17129.60 |
Organism: | Homo sapiens (Human) |
Description: | Amino acids 769-921 of human retinoblastoma 1. |
Residue: | 153 |
Sequence: | LQYASTRPPTLSPIPHIPRSPYKFPSSPLRIPGGNIYISPLKSPYKISEGLPTPTKMTPR
SRILVSIGESFGTSEKFQKINQMVCNSDRVLKRSAEGSNPPKPLKKLRFDIEGSDEADGS
KHLPGESKFQQKLAEMTSTRTRMQKQKMNDSMD
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