Molecule Details
InChIKeyBEUQXVWXFDOSAQ-UHFFFAOYSA-N
Compound NameTaselisib
Canonical SMILESCc1nc(-c2cn3c(n2)-c2ccc(-c4cnn(C(C)(C)C(N)=O)c4)cc2OCC3)n(C(C)C)n1
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)8
Pfam Stratification Cross-Family
Avg pChEMBL8.13
SourceBindingDB;ChEMBL
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB12108
Drug NameTaselisib
CAS Number1282512-48-4
Groups investigational
ATC Codes nan
DescriptionTaselisib has been used in trials studying the treatment and basic science of LYMPHOMA, Breast Cancer, Ovarian Cancer, Solid Neoplasm, and HER2/Neu Negative, among others.

Categories: Antineoplastic Agents Azepines Phosphatidylinositol 3-Kinases, antagonists & inhibitors
Cross-references: BindingDB: 50434806 CHEMBL2387080 ChemSpider: 29315044 PDB: 799 PharmGKB: PA166163227 PubChem:51001932 PubChem:347828409 Wikipedia: Taselisib ZINC: ZINC000068267049
Target Activities (8)
Target Gene Organism Category Pfam pChEMBL Type Source
P42336 PIK3CA Homo sapiens Human PF00454 PF00792 PF02192 PF00794 PF00613 9.5 Ki ChEMBL;BindingDB
O00329 PIK3CD Homo sapiens Human PF00454 PF00792 PF02192 PF00794 PF00613 9.4 Ki ChEMBL;BindingDB
P48736 PIK3CG Homo sapiens Human PF00454 PF00792 PF00794 PF00613 PF19710 9.0 Ki ChEMBL;BindingDB
P27986 PIK3R1 Homo sapiens Human PF16454 PF00620 PF00017 8.8 Ki BindingDB
P42338 PIK3CB Homo sapiens Human PF00454 PF00792 PF02192 PF00794 PF00613 8.0 Ki ChEMBL;BindingDB
O00459 PIK3R2 Homo sapiens Human PF16454 PF00620 PF00017 7.3 Ki ChEMBL;BindingDB
O00750 PIK3C2B Homo sapiens Human PF00168 PF00454 PF00792 PF00794 PF00613 PF00787 6.5 IC50 ChEMBL;BindingDB
Q8NEB9 PIK3C3 Homo sapiens Human PF00454 PF00792 PF00613 6.4 IC50 ChEMBL;BindingDB
DrugBank Target Actions (2)
Target Gene Target Name Action Type
P48736 PIK3CG Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform inhibitor targets
P42336 PIK3CA Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform modulator targets