Molecule Details
| InChIKey | PKCDDUHJAFVJJB-VLZXCDOPSA-N |
|---|---|
| Canonical SMILES | C[C@]1(O)C[C@@H](c2nc(-c3ccc4ccc(-c5ccccc5)nc4c3)c3c(N)nccn32)C1 |
| Clinical Status | Data-mined Candidate |
| Targets (Human+Pathogen) | 13 |
| Pfam Stratification | Cross-Family |
| Avg pChEMBL | 7.02 |
| Source | ChEMBL;BindingDB |
2D Structure
Activity Profile
DrugBank Annotations
| DrugBank ID | DB06075 |
|---|---|
| Drug Name | Linsitinib |
| CAS Number | 867160-71-2 |
| Groups | investigational |
| ATC Codes | nan |
| Description | An orally bioavailable small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. IGF-1R inhibitor OSI-906 selectively inhibits IGF-1R, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis... |
Cross-references: BindingDB: 50315887 CHEMBL1091644 Wikipedia: Linsitinib ZINC: ZINC000100071817
Target Activities (13)
| Target | Gene | Organism | Category | Pfam | pChEMBL | Type | Source |
|---|---|---|---|---|---|---|---|
| Q15759 | MAPK11 | Homo sapiens | Human | PF00069 | 8.0 | Kd | ChEMBL |
| P08069 | IGF1R | Homo sapiens | Human | PF00757 PF07714 PF01030 | 7.7 | IC50 | ChEMBL;BindingDB |
| P27361 | MAPK3 | Homo sapiens | Human | PF00069 | 7.5 | IC50 | ChEMBL |
| P28482 | MAPK1 | Homo sapiens | Human | PF00069 | 7.5 | IC50 | ChEMBL |
| P06213 | INSR | Homo sapiens | Human | PF00757 PF17870 PF07714 PF01030 | 7.3 | IC50 | ChEMBL;BindingDB |
| Q12851 | MAP4K2 | Homo sapiens | Human | PF00780 PF00069 | 7.2 | Kd | ChEMBL |
| P14616 | INSRR | Homo sapiens | Human | PF00041 PF00757 PF07714 PF01030 | 7.1 | IC50 | ChEMBL |
| O95835 | LATS1 | Homo sapiens | Human | PF00069 PF00433 PF00627 | 6.7 | Kd | ChEMBL |
| Q3MIX3 | ADCK5 | Homo sapiens | Human | PF03109 | 6.7 | Kd | ChEMBL |
| P36888 | FLT3 | Homo sapiens | Human | PF00047 PF07714 | 6.5 | Kd | ChEMBL |
| Q02750 | MAP2K1 | Homo sapiens | Human | PF00069 | 6.5 | Kd | ChEMBL |
| P08581 | MET | Homo sapiens | Human | PF07714 PF01437 PF01403 PF01833 | 6.4 | Kd | ChEMBL |
| Q9Y4K4 | MAP4K5 | Homo sapiens | Human | PF00780 PF00069 | 6.2 | Kd | ChEMBL |