Compound Detail
CHEMBL4216467
RIPRETINIB 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL4216467 |
| Name | RIPRETINIB |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | CEFJVGZHQAGLHS-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
2
Targets
7
Activities
1
Assay Types
0
PK Parameters
9
Publications
3
Known Names
2
Indications
2
Mechanisms
Molecular Properties
510.4
MW (Da)
5.67
ALogP
5
HBA
3
HBD
88.0
PSA (Ų)
0.32
QED
2
Ro5 Violations
5
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2020 |
| Availability | Prescription |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Stem cell growth factor receptor inhibitor | INHIBITOR | Mast/stem cell growth factor receptor Kit | ✓ | ✓ |
| Platelet-derived growth factor receptor alpha inhibitor | INHIBITOR | Platelet-derived growth factor receptor alpha | ✓ | ✓ |
Indications
Gastrointestinal Stromal Tumors Neoplasms
ATC Classification
L01EX19
ripretinib
Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Level 2: ANTINEOPLASTIC AGENTS
Activity Summary
IC50 7 meas. best 8.04
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Mast/stem cell growth factor receptor Kit CHEMBL1936 | IC50 | 8.04 | 7.0983 | 9.2 | 6 |
| Platelet-derived growth factor receptor alpha CHEMBL2007 | IC50 | 4.44 | 4.44 | 36000.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Mast/stem cell growth factor receptor Kit | IC50 | = | 9.2 | nM | 8.04 | Inhibition of KIT T670I mutant (unknown origin) | 36395392 |
| Mast/stem cell growth factor receptor Kit | IC50 | = | 13.0 | nM | 7.89 | Inhibition of wild type KIT (unknown origin) | 36395392 |
| Mast/stem cell growth factor receptor Kit | IC50 | = | 15.0 | nM | 7.82 | Inhibition of KIT (delta560 to 576 residues) deletion mutant autophosphorylation... | 36728508 |
| Mast/stem cell growth factor receptor Kit | IC50 | = | 31.0 | nM | 7.51 | Inhibition of KIT V654A mutant (unknown origin) by FRET based assay | 36728508 |
| Mast/stem cell growth factor receptor Kit | IC50 | = | 185.0 | nM | 6.73 | Inhibition of KIT (delta 560 to 576 residues) deletion/V654A double mutant autop... | 36728508 |
| Mast/stem cell growth factor receptor Kit | IC50 | = | 25000.0 | nM | 4.6 | Inhibition of KIT D816V mutant (unknown origin) | 36395392 |
| Platelet-derived growth factor receptor alpha | IC50 | = | 36000.0 | nM | 4.44 | Inhibition of PDGFRalpha D842V mutant (unknown origin) | 36395392 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 30204441 | 10.1021/acs.jmedchem.8b00938 | Mast/stem cell growth factor receptor Kit | 16 |
| 36395392 | 10.1021/acs.jmedchem.2c01361 | Mast/stem cell growth factor receptor Kit | 3 |
| 36728508 | 10.1021/acs.jmedchem.2c00851 | Mast/stem cell growth factor receptor Kit | 3 |
| 30204441 | 10.1021/acs.jmedchem.8b00938 | Platelet-derived growth factor receptor alpha | 2 |
| 30204441 | 10.1021/acs.jmedchem.8b00938 | BaF3 | 1 |
| 30204441 | 10.1021/acs.jmedchem.8b00938 | Vascular endothelial growth factor receptor 2 | 1 |
| 30204441 | 10.1021/acs.jmedchem.8b00938 | Unchecked | 1 |
| 30204441 | 10.1021/acs.jmedchem.8b00938 | Platelet-derived growth factor receptor beta | 1 |
| 36395392 | 10.1021/acs.jmedchem.2c01361 | Platelet-derived growth factor receptor alpha | 1 |
Data from ChEMBL 36 via Core Engine