Molecule Details
| InChIKey | QDITZBLZQQZVEE-YBEGLDIGSA-N |
|---|---|
| Compound Name | Gsk-1059615 |
| Canonical SMILES | O=C1NC(=O)/C(=C/c2ccc3nccc(-c4ccncc4)c3c2)S1 |
| Clinical Status | Data-mined Candidate |
| Targets (Human+Pathogen) | 19 |
| Pfam Stratification | Cross-Family |
| Avg pChEMBL | 7.56 |
| Source | ChEMBL |
2D Structure
Activity Profile
DrugBank Annotations
| DrugBank ID | DB11962 |
|---|---|
| Drug Name | GSK-1059615 |
| CAS Number | 958852-01-2 |
| Groups | investigational |
| ATC Codes | nan |
| Description | GSK1059615 has been used in trials studying the treatment of Lymphoma, Solid Tumours, Endometrial Cancer, Solid Tumor Cancer, and Metastatic Breast Cancer. |
Categories: mTOR Inhibitors
Cross-references: CHEMBL3544966 ChemSpider: 24747368 PubChem:23582824 PubChem:347828286 ZINC: ZINC000043176569
Target Activities (19)
| Target | Gene | Organism | Category | Pfam | pChEMBL | Type | Source |
|---|---|---|---|---|---|---|---|
| P42336 | PIK3CA | Homo sapiens | Human | PF00454 PF00792 PF02192 PF00794 PF00613 | 9.4 | IC50 | ChEMBL |
| P49760 | CLK2 | Homo sapiens | Human | PF00069 | 9.4 | Kd | ChEMBL |
| P42338 | PIK3CB | Homo sapiens | Human | PF00454 PF00792 PF02192 PF00794 PF00613 | 9.2 | IC50 | ChEMBL |
| O00329 | PIK3CD | Homo sapiens | Human | PF00454 PF00792 PF02192 PF00794 PF00613 | 8.7 | IC50 | ChEMBL |
| Q7L7X3 | TAOK1 | Homo sapiens | Human | PF00069 | 8.7 | Kd | ChEMBL |
| P48736 | PIK3CG | Homo sapiens | Human | PF00454 PF00792 PF00794 PF00613 PF19710 | 8.3 | IC50 | ChEMBL |
| P42345 | MTOR | Homo sapiens | Human | PF02259 PF02260 PF08771 PF23593 PF11865 PF00454 | 7.9 | IC50 | ChEMBL |
| P19784 | CSNK2A2 | Homo sapiens | Human | PF00069 | 7.8 | Kd | ChEMBL |
| P49759 | CLK1 | Homo sapiens | Human | PF00069 | 7.6 | Kd | ChEMBL |
| Q2M2I8 | AAK1 | Homo sapiens | Human | PF00069 | 7.5 | Kd | ChEMBL |
| Q96S44 | TP53RK | Homo sapiens | Human | PF06293 | 7.2 | Kd | ChEMBL |
| Q6ZSR9 | Homo sapiens | Human | PF15282 | 7.1 | Kd | ChEMBL | |
| P11309 | PIM1 | Homo sapiens | Human | PF00069 | 6.7 | Kd | ChEMBL |
| O94804 | STK10 | Homo sapiens | Human | PF00069 PF12474 | 6.5 | Kd | ChEMBL |
| Q13627 | DYRK1A | Homo sapiens | Human | PF00069 | 6.5 | Kd | ChEMBL |
| Q8TBX8 | PIP4K2C | Homo sapiens | Human | PF01504 | 6.5 | Kd | ChEMBL |
| Q9NSY1 | BMP2K | Homo sapiens | Human | PF15282 PF00069 | 6.4 | Kd | ChEMBL |
| O75676 | RPS6KA4 | Homo sapiens | Human | PF00069 PF00433 | 6.3 | Kd | ChEMBL |
| P78368 | CSNK1G2 | Homo sapiens | Human | PF12605 PF00069 | 6.0 | Kd | ChEMBL |
DrugBank Target Actions (3)
| Target | Gene | Target Name | Action | Type |
|---|---|---|---|---|
| P42345 | MTOR | Serine/threonine-protein kinase mTOR | inhibitor | targets |
| P48736 | PIK3CG | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | inhibitor | targets |
| Q8NEB9 | PIK3C3 | Phosphatidylinositol 3-kinase catalytic subunit type 3 | inhibitor | targets |