STX-478
Highest phase reached
Phase 1
Drug type
Small molecule
- Listing at source
- Listed
- Highest phase reached
- Phase 1
- Drug type
- Small molecule
- Drug name
- STX-478
- Molecular weight
- 401.3
- Structure (SMILES)
- Cc1c([C@@H](NC(=O)Nc2cnc(N)nc2)C(F)(F)F)oc2c(F)cc(F)cc12
- ly4064809
- LY4064809
- stx 478
- Stx-478
- STX-478
- tersolisib
- Tersolisib
- tersolisib [INN]
- TERSOLISIB [USAN]
- tersolisib inn
- tersolisib usan
- CAS registry numbers
- 2883540-92-7
- ChEMBL ID
- CHEMBL5421037
- InChIKey
- LGPNQALKGDDVBD-CYBMUJFWSA-N
- PubChem compound IDs
- 166532451
- FDA ingredient codes (UNII)
- AGX9NKC8M9
- First in class
- No
- Orphan designation
- No
- Pharmacology name
- tersolisib
- Type
- Synthetic organic
- Action type
- Inhibitor
- Target
- phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha
- Gene symbol
- phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha
- Gene symbol
- PIK3CA
- Protein identifier
- P42336
- Median affinity
- 7.15
- Affinity units
- pKd
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha
- Gene symbol
- PIK3CA
- Protein identifier
- P42336
- Median affinity
- 8.33
- Affinity units
- pKd
Open Targets indications
- Condition identifier
- MONDO_0007254
- Highest recorded phase
- 1
- Hydrogen bond acceptors
- 5
- Hydrogen bond donors
- 3
- Polar surface area
- 106.07
- Calculated partition coefficient (ALogP)
- 3.82
- Calculated partition coefficient (XLogP)
- 2.5
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 3
- Heavy atoms
- 28
- Molecular formula
- C16H12F5N5O2
- Monoisotopic mass
- 401.09111545
- Natural product
- No
- Recorded assays
- 61
- Active assays
- 3
Active assay types
- Confirmatory
Related records
Trials (8)
- A Study of [14C]-LY4064809 in Healthy Participants
- A Study of Food Effect and Esomeprazole on LY4064809 in Healthy Adult Participants
- A Study of Food Effect on Tersolisib (LY4064809) in Healthy Participants
- A Study of LY4064809 [14C]-STX-478 in Healthy Male Participants
- A Study of LY4064809 in Healthy Adult Chinese Participants
- A Study of LY4064809 in Healthy Adult Participants
- A Study of Tersolisib (LY4064809/STX-478) With Other Anti-Cancer Treatments in Participants With Advanced Breast Cancer With a Genetic Change (PIK3CA)
- First-in-Human Study of Tersolisib (STX-478) as Monotherapy and in Combination With Other Antineoplastic Agents in Participants With Advanced Solid Tumors