Bosmolisib

Highest phase reached
Drug type
Small molecule

Listing at source
Listed
Highest phase reached

Drug type
Small molecule
Drug name
Bosmolisib
Molecular weight
Structure (SMILES)
C[C@H](Nc1ncnc2[nH]ccc(=O)c12)c1c(Cl)c2cccc(Cl)c2c(=O)n1-c1ccccc1

  • 4 1s 1 4 8 dichloro 1 oxo 2 phenyl 3 isoquinolyl ethyl amino 8h pyrido 2 3 d pyrimidin 5 one
  • 4-[[(1S)-1-(4, 8-Dichloro-1-oxo-2-phenyl-3-isoquinolyl) ethyl] amino]-8H- pyrido[2,3-d] pyrimidin-5-one]
  • bosmolisib
  • Bosmolisib
  • bosmolisib [INN]
  • bosmolisib inn
  • br 101801
  • BR-101801
  • br101801
  • BR101801
  • BR101801 (Phase Ia)
  • BR101801 (Phase Ib)

CAS registry numbers
  • 2055765-77-8
ChEMBL ID
CHEMBL6068044
InChIKey
HIXUFHUKIOTXLJ-ZDUSSCGKSA-N
PubChem compound IDs
  • 134427646
FDA ingredient codes (UNII)
  • FJ5CTS1VNJ

First in class
No
Orphan designation
No

Pharmacology name
bosmolisib
Type
Synthetic organic
Drug name stem
-lisib

  • Action
    Inhibition
    Action type
    Inhibitor
    Target
    phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta
    Gene symbol
    PIK3CD
    Protein identifier
    O00329
    Median affinity
    8.7
    Affinity units
    pIC50
  • Action
    Inhibition
    Action type
    Inhibitor
    Target
    phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma
    Gene symbol
    PIK3CG
    Protein identifier
    P48736
    Median affinity
    7.82
    Affinity units
    pIC50

Investigated indications

  • Condition
    Neoplasms
    Highest recorded phase
    2
    Condition identifier
    EFO:0000616
    Subject identifier
    D009369

  • Condition identifier
    EFO_0000616
  • Condition identifier
    MONDO_0000430
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0004948
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0005070
  • Condition identifier
    MONDO_0015759
    Highest recorded phase
    1

Hydrogen bond acceptors
6
Hydrogen bond donors
2
Polar surface area
92.67
Calculated partition coefficient (ALogP)
5.1
Calculated partition coefficient (XLogP)
5.1
Prodrug
No
Chirality
Single enantiomer
Inorganic
No
Rule-of-five violations
1
Rotatable bonds
4
Heavy atoms
33
Molecular formula
C24H17Cl2N5O2
Monoisotopic mass
477.0759302
Natural product
No

Related records

Trials (15)

In development for (2)