Plixorafenib

Highest phase reached
Drug type
Small molecule

Listing at source
Listed
Highest phase reached

Drug type
Small molecule
Drug name
Plixorafenib
Molecular weight
Structure (SMILES)
O=C(c1c(F)ccc(NS(=O)(=O)N2CC[C@@H](F)C2)c1F)c1c[nH]c2ncc(-c3cnc(C4CC4)nc3)cc12

  • fore 8394
  • FORE-8394
  • fore8394
  • FORE8394
  • plixorafenib
  • Plixorafenib
  • plixorafenib [INN]
  • PLIXORAFENIB [USAN]
  • plixorafenib inn
  • plixorafenib usan
  • plx 8394
  • Plx 8394
  • PLX 8394 [WHO-DD]
  • plx 8394 who dd
  • Plx-8394
  • plx8394
  • PLX8394

CAS registry numbers
  • 1393466-87-9
ChEMBL ID
CHEMBL4303729
InChIKey
YYACLQUDUDXAPA-MRXNPFEDSA-N
PubChem compound IDs
  • 90116675
FDA ingredient codes (UNII)
  • J2L7Z273SG

First in class
No
Orphan designation
No

Pharmacology name
plixorafenib
Type
Synthetic organic
Drug name stem
-rafenib

  • Action
    Inhibition
    Action type
    Inhibitor
    Target
    Raf-1 proto-oncogene, serine/threonine kinase
    Gene symbol
    RAF1
    Protein identifier
    P04049
    Median affinity
    7.64
    Affinity units
    pIC50
  • Action
    Inhibition
    Action type
    Inhibitor
    Target
    B-Raf proto-oncogene, serine/threonine kinase
    Gene symbol
    BRAF
    Protein identifier
    P15056
    Median affinity
    7.85
    Affinity units
    pIC50
  • Mechanism
    Serine/threonine-protein kinase B-raf inhibitor
    Action type
    Inhibitor
    Target
    Serine/threonine-protein kinase B-raf
    Protein identifier
    P15056

Open Targets mechanisms

  • Mechanism
    Serine/threonine-protein kinase B-raf inhibitor
    Action type
    Inhibitor
    Target
    Serine/threonine-protein kinase B-raf

  • Condition
    Neoplasms
    Highest recorded phase
    2
    Condition identifier
    EFO:0000616
    Subject identifier
    D009369
  • Condition
    Melanoma
    Highest recorded phase
    1
    Condition identifier
    EFO:0000756
    Subject identifier
    D008545
  • Condition
    Carcinoma, Non-Small-Cell Lung
    Highest recorded phase
    1
    Condition identifier
    EFO:0003060
    Subject identifier
    D002289
  • Condition
    Cholangiocarcinoma
    Highest recorded phase
    1
    Condition identifier
    EFO:0005221
    Subject identifier
    D018281
  • Condition
    Leukemia, Hairy Cell
    Highest recorded phase
    1
    Condition identifier
    EFO:1000956
    Subject identifier
    D007943
  • Condition
    Histiocytosis
    Highest recorded phase
    1
    Condition identifier
    HP:0100727
    Subject identifier
    D015614
  • Condition
    Thyroid Neoplasms
    Highest recorded phase
    1
    Condition identifier
    MONDO:0002108
    Subject identifier
    D013964
  • Condition
    Neoplasms
    Highest recorded phase
    2
    Condition identifier
    MONDO:0004992
    Subject identifier
    D009369
  • Condition
    Colorectal Neoplasms
    Highest recorded phase
    1
    Condition identifier
    MONDO:0005575
    Subject identifier
    D015179

  • Condition identifier
    EFO_0000616
  • Condition identifier
    EFO_0000756
  • Condition identifier
    EFO_0003060
    Highest recorded phase
    1
  • Condition identifier
    EFO_0005221
    Highest recorded phase
    1
  • Condition identifier
    EFO_1000956
    Highest recorded phase
    1
  • Condition identifier
    HP_0100727
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0002108
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0002108
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0004992
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0005070
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0005105
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0005575
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0018935
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0021042
    Highest recorded phase
    1

Hydrogen bond acceptors
6
Hydrogen bond donors
2
Polar surface area
120.94
Calculated partition coefficient (ALogP)
4.11
Calculated partition coefficient (XLogP)
2.8
Prodrug
No
Chirality
Single enantiomer
Inorganic
No
Rule-of-five violations
1
Rotatable bonds
7
Heavy atoms
38
Molecular formula
C25H21F3N6O3S
Monoisotopic mass
542.13479421
Natural product
No

Recorded assays
331
Active assays
60

  • Confirmatory
  • Other
  • Screening

Related records

Trials (6)

In development for (10)

Targets (2)