Azenosertib

Highest phase reached
Drug type
Small molecule

Listing at source
Listed
Highest phase reached

Drug type
Small molecule
Drug name
Azenosertib
Molecular weight
Structure (SMILES)
C=CCn1c(=O)c2cnc(Nc3ccc(N4CCN(C)CC4)cc3)nc2n1-c1ccc2c(n1)[C@@](O)(CC)CC2

  • azenosertib
  • Azenosertib
  • Azenosertib [INN]
  • Azenosertib [WHO-DD]
  • azenosertib inn
  • azenosertib who dd
  • zn c3
  • Zn-c3
  • ZN-c3
  • ZN-C3

CAS registry numbers
  • 2376146-48-2
ChEMBL ID
CHEMBL5095036
InChIKey
OXTSYWDBUVRXFF-GDLZYMKVSA-N
PubChem compound IDs
  • 139467635
FDA ingredient codes (UNII)
  • 9J13XU96Z1

First in class
No
Orphan designation
No

Pharmacology name
azenosertib
Type
Synthetic organic
Drug name stem
-sertib

  • Action
    Inhibition
    Action type
    Inhibitor
    Target
    WEE1 G2 checkpoint kinase
    Gene symbol
    WEE1
    Protein identifier
    P30291
    Median affinity
    8.41
    Affinity units
    pIC50
  • Mechanism
    Serine/threonine-protein kinase WEE1 inhibitor
    Action type
    Inhibitor
    Target
    Wee1-like protein kinase
    Protein identifier
    P30291

Open Targets mechanisms

  • Mechanism
    Serine/threonine-protein kinase WEE1 inhibitor
    Action type
    Inhibitor
    Target
    Wee1-like protein kinase

  • Condition
    Neoplasms
    Highest recorded phase
    2
    Condition identifier
    EFO:0000616
    Subject identifier
    D009369
  • Condition
    Osteosarcoma
    Highest recorded phase
    1
    Condition identifier
    EFO:0000637
    Subject identifier
    D012516
  • Condition
    Pancreatic Neoplasms
    Highest recorded phase
    0.5
    Condition identifier
    EFO:0002618
    Subject identifier
    D010190
  • Condition
    Leukemia, Myeloid
    Highest recorded phase
    1
    Condition identifier
    MONDO:0004643
    Subject identifier
    D007951
  • Condition
    Carcinoma, Pancreatic Ductal
    Highest recorded phase
    0.5
    Condition identifier
    MONDO:0005184
    Subject identifier
    D021441

  • Condition identifier
    EFO_0000616
    Highest recorded phase
    1
  • Condition identifier
    EFO_1000238
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0001056
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0002087
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0002158
    Highest recorded phase
    3
  • Condition identifier
    MONDO_0004643
  • Condition identifier
    MONDO_0004992
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0005070
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0005140
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0005184
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0005494
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0005575
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0006047
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0006196
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0007254
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0008170
    Highest recorded phase
    3
  • Condition identifier
    MONDO_0009807
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0015686
    Highest recorded phase
    3
  • Condition identifier
    MONDO_0018874
    Highest recorded phase
    1

Hydrogen bond acceptors
10
Hydrogen bond donors
2
Polar surface area
104.34
Calculated partition coefficient (ALogP)
3.2
Calculated partition coefficient (XLogP)
3.7
Prodrug
No
Chirality
Single enantiomer
Inorganic
No
Rule-of-five violations
1
Rotatable bonds
7
Heavy atoms
39
Molecular formula
C29H34N8O2
Monoisotopic mass
526.28047236
Natural product
No

Recorded assays
136
Active assays
80

Active assay types

  • Confirmatory

Related records

Trials (16)

In development for (6)

Targets (1)