Details of the Drug Combination

General Information of Drug Combination (ID: DCFP548)

Drug Combination Name
Picoplatin SCH 727965
Indication
Disease Entry Status REF
Colon adenocarcinoma Investigative [1]
Component Drugs Picoplatin   DM0PIY6 SCH 727965   DMCJLD1
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL 3D MOL
High-throughput Screening Result Testing Cell Line: COLO 205
Zero Interaction Potency (ZIP) Score: 7.81
Bliss Independence Score: 9.16
Loewe Additivity Score: 2.02
LHighest Single Agent (HSA) Score: 1.82

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of Picoplatin
Disease Entry ICD 11 Status REF
Colorectal cancer 2B91.Z Phase 3 [2]
Ovarian cancer 2C73 Phase 3 [2]
Prostate cancer 2C82.0 Phase 3 [2]
Small-cell lung cancer 2C25.Y Phase 3 [2]
Indication(s) of SCH 727965
Disease Entry ICD 11 Status REF
Acute lymphoblastic leukaemia 2A85 Discontinued in Phase 3 [3]
SCH 727965 Interacts with 3 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Cyclin-dependent kinase 9 (CDK9) TT1LVF2 CDK9_HUMAN Inhibitor [4]
Cyclin-dependent kinase 1 (CDK1) TTH6V3D CDK1_HUMAN Inhibitor [4]
Cyclin-dependent kinase 2 (CDK2) TT7HF4W CDK2_HUMAN Inhibitor [4]
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SCH 727965 Interacts with 4 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Retinoblastoma-associated protein (RB1) OTQJUJMZ RB_HUMAN Decreases Phosphorylation [5]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Increases Cleavage [5]
Breast cancer type 1 susceptibility protein (BRCA1) OT5BN6VH BRCA1_HUMAN Decreases Expression [6]
Fanconi anemia group D2 protein (FANCD2) OTVEB5LF FACD2_HUMAN Decreases Expression [6]
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Test Results of This Drug Combination in Other Disease Systems

Indication DrugCom ID Cell Line Status REF
Glioma DC9T9IU SF-268 Investigative [7]
Carcinoma DCV2428 RXF 393 Investigative [1]
Adenocarcinoma DCCZVZ5 A549 Investigative [8]
Adenocarcinoma DCC1NRT NCIH23 Investigative [8]
Cutaneous melanoma DC720PE SK-MEL-5 Investigative [8]
Large cell lung carcinoma DCR2ESQ NCI-H460 Investigative [8]
Lung adenocarcinoma DCSP3L4 MDA-MB-231 Investigative [8]
Lung adenocarcinoma DC5N9FC HOP-62 Investigative [8]
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⏷ Show the Full List of 8 DrugCom(s)

References

1 CheMBL Affinity Phenotypic Cellular Interaction Assay ID: CHEMBL1126165
2 ClinicalTrials.gov (NCT00465491) Study of Picoplatin Efficacy After Relapse. U.S. National Institutes of Health.
3 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7379).
4 Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
5 Dinaciclib (SCH 727965), a novel and potent cyclin-dependent kinase inhibitor. Mol Cancer Ther. 2010 Aug;9(8):2344-53. doi: 10.1158/1535-7163.MCT-10-0324. Epub 2010 Jul 27.
6 CDK12 Inhibition Reverses De Novo and Acquired PARP Inhibitor Resistance in BRCA Wild-Type and Mutated Models of Triple-Negative Breast Cancer. Cell Rep. 2016 Nov 22;17(9):2367-2381. doi: 10.1016/j.celrep.2016.10.077.
7 CheMBL Affinity Phenotypic Cellular Interaction Assay ID: CHEMBL1125966
8 CheMBL Affinity Phenotypic Cellular Interaction Assay ID: CHEMBL1125976