Fazamorexant

Highest phase reached
Drug type
Small molecule

Listing at source
Listed
Highest phase reached

Drug type
Small molecule
Drug name
Fazamorexant
Molecular weight
Structure (SMILES)
Cc1ccc(-c2ncccn2)c(C(=O)N2[C@H]3CC[C@@H](COc4ccc(F)cn4)[C@@H]2CC3)c1

  • fazamorexant
  • Fazamorexant
  • fazamorexant [INN]
  • fazamorexant inn
  • yzj 1139
  • YZJ-1139
  • YZJ-1139 10mg
  • YZJ-1139 20mg
  • YZJ-1139 40mg
  • YZJ-1139 60mg
  • YZJ-1139 tablets

CAS registry numbers
  • 1808918-69-5
ChEMBL ID
CHEMBL5314459
InChIKey
PMJPLAGTPPVSRL-JLMWRMLUSA-N
PubChem compound IDs
  • 156889652
FDA ingredient codes (UNII)
  • MDH4D7M594

First in class
No
Orphan designation
No

Pharmacology name
fazamorexant
Type
Synthetic organic

  • Action
    Antagonist
    Action type
    Antagonist
    Target
    OX1 receptor
    Gene symbol
    HCRTR1
    Protein identifier
    O43613
    Median affinity
    7.7
    Affinity units
    pIC50
  • Action
    Antagonist
    Action type
    Antagonist
    Target
    OX2 receptor
    Gene symbol
    HCRTR2
    Protein identifier
    O43614
    Median affinity
    7.44
    Affinity units
    pIC50

Investigated indications

  • Condition
    Sleep Initiation and Maintenance Disorders
    Highest recorded phase
    3
    Condition identifier
    EFO:0004698
    Subject identifier
    D007319

  • Condition identifier
    EFO_0004698
    Highest recorded phase
    3
  • Condition identifier
    MONDO_0013600
    Highest recorded phase
    3

Trial references

Hydrogen bond acceptors
5
Hydrogen bond donors
0
Polar surface area
68.21
Calculated partition coefficient (ALogP)
4.45
Calculated partition coefficient (XLogP)
4.1
Prodrug
No
Chirality
Single enantiomer
Inorganic
No
Rule-of-five violations
0
Rotatable bonds
5
Heavy atoms
32
Molecular formula
C25H25FN4O2
Monoisotopic mass
432.19615422
Natural product
No

Related records

Trials (9)

In development for (1)