Reaction Details |
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Target | Cyclin-dependent kinase 4/G1/S-specific cyclin-D1 |
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Ligand | BDBM6861 |
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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 | 16200±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 4/G1/S-specific cyclin-D1 |
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Name: | Cyclin-dependent kinase 4/G1/S-specific cyclin-D1 |
Synonyms: | CDK4/CycD | CDK4/CycD1 | CDK4/Cyclin D1 | CDK4/D1 | Cyclin-Dependent Kinase 4 (CDK4) | Cyclin-dependent kinase 4 | Cyclin-dependent kinase 4/G1/S-specific cyclin D1 | Cyclin-dependent kinase 4/cyclin D1 |
Type: | Protein Complex |
Mol. Mass.: | n/a |
Description: | CDK4/D1 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 |
Synonyms: | B-cell lymphoma 1 protein | BCL-1 | BCL-1 oncogene | BCL1 | CCND1 | CCND1_HUMAN | PRAD1 | PRAD1 oncogene |
Type: | Enzyme Subunit |
Mol. Mass.: | 33717.70 |
Organism: | Homo sapiens (Human) |
Description: | n/a |
Residue: | 295 |
Sequence: | MEHQLLCCEVETIRRAYPDANLLNDRVLRAMLKAEETCAPSVSYFKCVQKEVLPSMRKIV
ATWMLEVCEEQKCEEEVFPLAMNYLDRFLSLEPVKKSRLQLLGATCMFVASKMKETIPLT
AEKLCIYTDNSIRPEELLQMELLLVNKLKWNLAAMTPHDFIEHFLSKMPEAEENKQIIRK
HAQTFVALCATDVKFISNPPSMVAAGSVVAAVQGLNLRSPNNFLSYYRLTRFLSRVIKCD
PDCLRACQEQIEALLESSLRQAQQNMDPKAAEEEEEEEEEVDLACTPTDVRDVDI
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BDBM6861 |
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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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