Molecule Details
| InChIKey | HVIGNZUDBVLTLU-MRXNPFEDSA-N |
|---|---|
| Compound Name | Tizaterkib |
| Canonical SMILES | COC[C@H]1Cn2cc(-c3nc(Nc4ccnn4C)ncc3C)nc2C(=O)N1Cc1ccc(F)c(F)c1 |
| Clinical Status | Data-mined Candidate |
| Targets (Human+Pathogen) | 7 |
| Pfam Stratification | Cross-Family |
| Avg pChEMBL | 7.02 |
| Source | ChEMBL;BindingDB |
2D Structure
Activity Profile
DrugBank Annotations
| DrugBank ID | DB21296 |
|---|---|
| Drug Name | Tizaterkib |
| CAS Number | 2097416-76-5 |
| Groups | investigational |
| ATC Codes | nan |
| Description | Tizaterkib is a small molecule drug. The usage of the INN stem '-terkib' in the name indicates that Tizaterkib is a extracellular signal-regulated kinase (ERK) inhibitor. Tizaterkib is under investigation in clinical trial NCT04305249 (Safety and Preliminary Efficacy of ATG-017 Monotherapy or Combin... |
Cross-references: BindingDB: 50505988 CHEMBL4482864 PDB: LHZ
Target Activities (7)
| Target | Gene | Organism | Category | Pfam | pChEMBL | Type | Source |
|---|---|---|---|---|---|---|---|
| P28482 | MAPK1 | Homo sapiens | Human | PF00069 | 9.2 | IC50 | ChEMBL;BindingDB |
| P27361 | MAPK3 | Homo sapiens | Human | PF00069 | 8.5 | IC50 | ChEMBL |
| Q00535 | CDK5 | Homo sapiens | Human | PF00069 | 6.5 | IC50 | ChEMBL |
| Q15078 | CDK5R1 | Homo sapiens | Human | PF03261 | 6.5 | IC50 | ChEMBL;BindingDB |
| O60285 | NUAK1 | Homo sapiens | Human | PF00069 | 6.4 | IC50 | ChEMBL;BindingDB |
| P24864 | CCNE1 | Homo sapiens | Human | PF02984 PF00134 | 6.0 | IC50 | ChEMBL |
| P24941 | CDK2 | Homo sapiens | Human | PF00069 | 6.0 | IC50 | ChEMBL;BindingDB |