Reaction Details |
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Target | Cyclin-dependent kinase 4/G1/S-specific cyclin-D1 |
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Ligand | BDBM6309 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1656373 (CHEMBL4005843) |
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Ki | 3.0±n/a nM |
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Citation | Tadesse, S; Yu, M; Mekonnen, LB; Lam, F; Islam, S; Tomusange, K; Rahaman, MH; Noll, B; Basnet, SK; Teo, T; Albrecht, H; Milne, R; Wang, S Highly Potent, Selective, and Orally Bioavailable 4-Thiazol-N-(pyridin-2-yl)pyrimidin-2-amine Cyclin-Dependent Kinases 4 and 6 Inhibitors as Anticancer Drug Candidates: Design, Synthesis, and Evaluation. J Med Chem60:1892-1915 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, 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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BDBM6309 |
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n/a |
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Name | BDBM6309 |
Synonyms: | 6-Acetyl-8-cyclopentyl-5-methyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one Hydrochloride | 8-cyclopentyl-6-acetyl-5-methyl-2-{[5-(piperazin-1-yl)pyridin-2-yl]amino}-7H,8H-pyrido[2,3-d]pyrimidin-7-one | Ibrance | PD 0332991 | Palbociclib | Pyrido-[2,3-d]-pyrimidin-7-one 43 | US10189849, PD0332991 | US10464927, Compound Palbociclib | US10626107, Example Palbociclib | US10696682, Compound PD0332991 | US10927120, PD0332991 | US9464092, PD0332991 | US9957276, PD0332991 |
Type | Small organic molecule |
Emp. Form. | C24H29N7O2 |
Mol. Mass. | 447.5328 |
SMILES | CC(=O)c1c(C)c2cnc(Nc3ccc(cn3)N3CCNCC3)nc2n(C2CCCC2)c1=O |
Structure |
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