IDRX-42
Highest phase reached
Phase 1
Drug type
Small molecule
- Listing at source
- Listed
- Highest phase reached
- Phase 1
- Drug type
- Small molecule
- Drug name
- IDRX-42
- Molecular weight
- 508.63
- Structure (SMILES)
- Cn1cc(-c2ccc(CNc3cc(-c4cnc5cc(OCCCN6CCCC6)ccn45)ncn3)cc2)cn1
- idrx 42
- Idrx-42
- IDRX-42
- m 4205
- M-4205
- velzatinib
- Velzatinib
- velzatinib [INN]
- velzatinib inn
- CAS registry numbers
- 2590556-80-0
- ChEMBL ID
- CHEMBL5314917
- InChIKey
- LVMAULGVWBINFP-UHFFFAOYSA-N
- PubChem compound IDs
- 155587867
- FDA ingredient codes (UNII)
- Y6UHU32G5Z
- First in class
- No
- Orphan designation
- No
- Pharmacology name
- velzatinib
- Type
- Synthetic organic
- Action type
- Inhibitor
- Target
- colony stimulating factor 1 receptor
- Gene symbol
- colony stimulating factor 1 receptor
- Action type
- Inhibitor
- Target
- KIT proto-oncogene, receptor tyrosine kinase
- Gene symbol
- KIT proto-oncogene, receptor tyrosine kinase
- Action type
- Inhibitor
- Target
- platelet derived growth factor receptor alpha
- Gene symbol
- platelet derived growth factor receptor alpha
- Action type
- Inhibitor
- Target
- platelet derived growth factor receptor beta
- Gene symbol
- platelet derived growth factor receptor beta
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- colony stimulating factor 1 receptor
- Gene symbol
- CSF1R
- Protein identifier
- P07333
- Median affinity
- 8.26
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- platelet derived growth factor receptor beta
- Gene symbol
- PDGFRB
- Protein identifier
- P09619
- Median affinity
- 8.59
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- KIT proto-oncogene, receptor tyrosine kinase
- Gene symbol
- KIT
- Protein identifier
- P10721
- Median affinity
- 7.36
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- platelet derived growth factor receptor alpha
- Gene symbol
- PDGFRA
- Protein identifier
- P16234
- Median affinity
- 7.3
- Affinity units
- pIC50
Open Targets indications
- Condition identifier
- MONDO_0011719
- Highest recorded phase
- 3
- Hydrogen bond acceptors
- 9
- Hydrogen bond donors
- 1
- Polar surface area
- 85.4
- Calculated partition coefficient (ALogP)
- 4.67
- Calculated partition coefficient (XLogP)
- 4.3
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 1
- Rotatable bonds
- 10
- Heavy atoms
- 38
- Molecular formula
- C29H32N8O
- Monoisotopic mass
- 508.26990767
- Natural product
- No
- Recorded assays
- 164
- Active assays
- 10
Active assay types
- Confirmatory
These details could not be displayed.
Related records
Trials (4)
- A Study of IDRX-42 (GSK6042981) Versus (vs) Sunitinib in Participants With Gastrointestinal Stromal Tumors After Imatinib Therapy
- A Study of Velzatinib in Participants With Metastatic and/or Unresectable GIST After Imatinib, Sunitinib, Regorafenib, and Pimitespib
- A Study to Investigate Velzatinib Compared With Imatinib in Adult Participants With Previously Untreated Metastatic and/or Unresectable Gastrointestinal Stromal Tumors (StrateGIST Frontline)
- First-in-human Study of IDRX-42 in Participants With Metastatic and/or Unresectable Gastrointestinal Stromal Tumors