Molecule Details
InChIKeyVXBAJLGYBMTJCY-NSCUHMNNSA-N
Compound NameZotiraciclib
Canonical SMILESCN1C/C=C/CCOc2cccc(c2)-c2ccnc(n2)Nc2cccc(c2)C1
Clinical Status Clinical Multi-Target
Targets (Human+Pathogen)34
Pfam Stratification Cross-Family
Avg pChEMBL7.27
SourceChEMBL;BindingDB;TTD_MultiTarget
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB16656
Drug NameZotiraciclib
CAS Number1204918-72-8
Groups investigational
ATC Codes nan
DescriptionZotiraciclib is under investigation in clinical trial NCT02942264 (Zotiraciclib (TG02) Plus Dose-dense or Metronomic Temozolomide Followed by Randomized Phase II Trial of Zotiraciclib (TG02) Plus Temozolomide Versus Temozolomide Alone in Adults With Recurrent Anaplastic Astrocytoma and Glioblastoma)...

Categories: Cyclin-Dependent Kinases, antagonists & inhibitors Heterocyclic Compounds, Fused-Ring
Cross-references: BindingDB: 50363196 CHEMBL1944698 ChemSpider: 20571045 Wikipedia: Zotiraciclib ZINC: ZINC000068251500
Target Activities (34)
Target Gene Organism Category Pfam pChEMBL Type Source
P50750 CDK9 Homo sapiens Human PF00069 8.6 IC50 ChEMBL;BindingDB
O75909 CCNK Homo sapiens Human PF00134 PF21797 8.5 IC50 ChEMBL;BindingDB
Q00535 CDK5 Homo sapiens Human PF00069 8.4 IC50 ChEMBL;BindingDB
Q15078 CDK5R1 Homo sapiens Human PF03261 8.4 IC50 ChEMBL;BindingDB
P24864 CCNE1 Homo sapiens Human PF02984 PF00134 8.1 IC50 ChEMBL;BindingDB
Q00526 CDK3 Homo sapiens Human PF00069 8.1 IC50 ChEMBL
P06493 CDK1 Homo sapiens Human PF00069 8.1 IC50 ChEMBL;BindingDB
P14635 CCNB1 Homo sapiens Human PF02984 PF00134 8.1 IC50 ChEMBL
P51946 CCNH Homo sapiens Human PF16899 PF00134 8.0 IC50 ChEMBL;BindingDB
P51948 MNAT1 Homo sapiens Human PF25811 PF06391 PF17121 8.0 IC50 ChEMBL
P20248 CCNA2 Homo sapiens Human PF02984 PF00134 PF16500 7.9 IC50 ChEMBL
P24941 CDK2 Homo sapiens Human PF00069 7.9 pIC50 TTD_MultiTarget
P78396 CCNA1 Homo sapiens Human PF02984 PF00134 PF16500 7.9 IC50 ChEMBL
Q86TW2 ADCK1 Homo sapiens Human PF03109 7.6 Kd ChEMBL
Q02161 RHD Homo sapiens Human PF00909 7.5 pIC50 TTD_MultiTarget
Q00536 CDK16 Homo sapiens Human PF00069 7.5 Kd ChEMBL
P50613 CDK7 Homo sapiens Human PF00069 7.4 IC50 ChEMBL;BindingDB
Q13164 MAPK7 Homo sapiens Human PF00069 7.4 IC50 ChEMBL
P36888 FLT3 Homo sapiens Human PF00047 PF07714 7.2 IC50 ChEMBL;BindingDB
O60674 JAK2 Homo sapiens Human PF18379 PF18377 PF17887 PF07714 PF21990 7.1 IC50 ChEMBL;BindingDB
P18505 GABRB1 Homo sapiens Human PF02931 PF02932 7.1 pIC50 TTD_MultiTarget
Q16513 PKN2 Homo sapiens Human PF02185 PF00069 PF00433 6.8 Kd ChEMBL
P22830 FECH Homo sapiens Human PF00762 6.6 Kd ChEMBL
Q9Y616 IRAK3 Homo sapiens Human PF00531 PF00069 6.5 Kd ChEMBL
Q13188 STK3 Homo sapiens Human PF11629 PF00069 6.5 Kd ChEMBL
P18074 ERCC2 Homo sapiens Human PF06733 PF06777 PF13307 6.5 Kd ChEMBL
P49841 GSK3B Homo sapiens Human PF00069 6.3 Kd ChEMBL
Q9BZL6 PRKD2 Homo sapiens Human PF00130 PF00169 PF00069 PF25525 6.3 Kd ChEMBL
O94806 PRKD3 Homo sapiens Human PF00130 PF00169 PF00069 PF25525 6.2 Kd ChEMBL
P49840 GSK3A Homo sapiens Human PF00069 6.2 Kd ChEMBL
Q8IVH8 MAP4K3 Homo sapiens Human PF00780 PF00069 6.1 Kd ChEMBL
P17252 PRKCA Homo sapiens Human PF00130 PF00168 PF00069 PF00433 6.0 Kd ChEMBL
P10635 CYP2D6 Homo sapiens Human PF00067 6.0 IC50 ChEMBL;BindingDB
Q05655 PRKCD Homo sapiens Human PF00130 PF21494 PF00069 PF00433 6.0 Kd ChEMBL
DrugBank Target Actions (4)
Target Gene Target Name Action Type
P06239 LCK Tyrosine-protein kinase Lck inhibitor targets
P06241 FYN Tyrosine-protein kinase Fyn inhibitor targets
P50750 CDK9 Cyclin-dependent kinase 9 inhibitor targets
P24941 CDK2 Cyclin-dependent kinase 2 modulator targets