Aticaprant
Highest phase reached
Phase 3
Drug type
Small molecule
- Listing at source
- Listed
- Highest phase reached
- Phase 3
- Drug type
- Small molecule
- Drug name
- Aticaprant
- Molecular weight
- 418.51
- Structure (SMILES)
- Cc1cc(C)cc([C@@H]2CCCN2Cc2ccc(Oc3ccc(C(N)=O)cc3F)cc2)c1
- aticaprant
- Aticaprant
- aticaprant [INN]
- ATICAPRANT [USAN]
- Aticaprant [WHO-DD]
- aticaprant inn
- aticaprant usan
- aticaprant who dd
- cerc 501
- Cerc-501
- CERC-501
- jnj 67953964
- jnj 67953964 aaa
- Jnj-67953964
- JNJ-67953964
- JNJ-67953964-AAA
- jspa 0658
- JSPA-0658
- jspa0658
- JSPA0658
- ly 2456302
- LY-2456302
- ly2456302
- Ly2456302
- LY2456302
- CAS registry numbers
- 1174130-61-0
- ChEMBL ID
- CHEMBL1921847
- InChIKey
- ZHPMYDSXGRRERG-DEOSSOPVSA-N
- PubChem compound IDs
- 44129648
- FDA ingredient codes (UNII)
- DE4G8X55F5
- First in class
- No
- Orphan designation
- No
- Pharmacology name
- aticaprant
- Type
- Synthetic organic
- Drug name stem
- -caprant
- Action
- Antagonist
- Action type
- Antagonist
- Target
- μ receptor
- Gene symbol
- OPRM1
- Protein identifier
- P35372
- Median affinity
- 7.62
- Affinity units
- pKi
- Action
- Antagonist
- Action type
- Antagonist
- Target
- δ receptor
- Gene symbol
- OPRD1
- Protein identifier
- P41143
- Median affinity
- 6.81
- Affinity units
- pKi
- Action
- Antagonist
- Action type
- Antagonist
- Target
- κ receptor
- Gene symbol
- OPRK1
- Protein identifier
- P41145
- Median affinity
- 9.09
- Affinity units
- pKB
- Primary target
- Yes
- Action
- Antagonist
- Action type
- Antagonist
- Target
- κ receptor
- Gene symbol
- OPRK1
- Protein identifier
- P41145
- Median affinity
- 9.09
- Affinity units
- pKi
- Primary target
- Yes
- Mechanism
- Kappa opioid receptor antagonist
- Action type
- Antagonist
- Target
- Kappa-type opioid receptor
- Protein identifier
- P41145
Open Targets mechanisms
- Mechanism
- Kappa opioid receptor antagonist
- Action type
- Antagonist
- Target
- Kappa-type opioid receptor
- Condition
- Depressive Disorder, Major
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003761
- Subject identifier
- D003865
- Condition
- Tobacco Use Disorder
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003768
- Subject identifier
- D014029
- Condition
- Anxiety
- Highest recorded phase
- 1
- Condition identifier
- EFO:0005230
- Subject identifier
- D001007
- Condition
- Depressive Disorder, Treatment-Resistant
- Highest recorded phase
- 2
- Condition identifier
- EFO:0009854
- Subject identifier
- D061218
- Condition
- Depressive Disorder, Major
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0002009
- Subject identifier
- D003865
- Condition identifier
- EFO_0003768
- Highest recorded phase
- 2
- Condition identifier
- EFO_0004318
- Highest recorded phase
- 2
- Condition identifier
- EFO_0009854
- Highest recorded phase
- 2
- Condition identifier
- HP_0000739
- Highest recorded phase
- 1
- Condition identifier
- HP_0000739
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0001247
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0001442
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0001942
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002009
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0002050
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004985
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005146
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005371
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005383
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0007079
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0008114
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0008575
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0011918
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0012000
- Highest recorded phase
- 2
- NCT01913535
- NCT02218775
- NCT02641028
- NCT02800928
- NCT03559192
- NCT05518149
- Hydrogen bond acceptors
- 3
- Hydrogen bond donors
- 1
- Polar surface area
- 55.56
- Calculated partition coefficient (ALogP)
- 5.67
- Calculated partition coefficient (XLogP)
- 5
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 1
- Rotatable bonds
- 6
- Heavy atoms
- 31
- Molecular formula
- C26H27FN2O2
- Monoisotopic mass
- 418.20565627
- Natural product
- No
- Recorded assays
- 65
- Active assays
- 23
- Confirmatory
- Other
- Narcotic Antagonists
Oral bioavailability
- Median
- 25.2
- Mean
- 25.2
- Minimum
- 25
- Maximum
- 25.4
- Unit
- %
- Assays
- 4
- Standard deviation
- 0.23094
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- F
Related records
Trials (16)
- A Study in a Human Laboratory Model of Smoking Behavior
- A Study of 14C JNJ-67953964 in Healthy Adult Male Participants
- A Study of Aticaprant 10 mg as Adjunctive Therapy in Adult Participants With Major Depressive Disorder (MDD) With Moderate-to-severe Anhedonia and Inadequate Response to Current Antidepressant Therapy and Long-term Extension Treatment With Aticaprant
- A Study of Aticaprant 10 Milligrams (mg) as Adjunctive Therapy in Adult Participants With MDD With Moderate-to-severe Anhedonia and Inadequate Response to Current Antidepressant Therapy
- A Study of Aticaprant as Adjunctive Therapy in Adult Participants With Major Depressive Disorder (MDD) With Moderate-to-severe Anhedonia and Inadequate Response to Current Antidepressant Therapy
- A Study of Aticaprant in Adult and Elderly Participants With Major Depressive Disorder (MDD)
- A Study of Aticaprant Plus an Antidepressant to Prevent Return of Depression Symptoms in Participants With Major Depressive Disorder Who Experience a Loss of Interest and Pleasure
- A Study of JNJ-67953964 in Healthy Japanese Adult Male Participants
- A Study of the Feasibility, Safety and Tolerability of Aticaprant as Adjunctive Treatment in Participants With Schizophrenia
- A Study to Explore the Efficacy of JNJ-67953964 in the Treatment of Depression
- A Study to Investigate the Effect of JNJ-67953964 on Gastric Mucosal Integrity in Healthy Male and Female Participants
- A Thorough QT Study of Aticaprant (JNJ-67953964) in Healthy Adult Participants
- Does CERC-501 Attenuate Stress-precipitated Smoking Lapse?
- Fast-Fail Trials in Mood and Anxiety Spectrum Disorders; Kappa Opioid Receptor Phase 2a
- FASTMAS (Fast-Fail Trials in Mood and Anxiety Spectrum Disorders) Kappa Opioid Receptor Phase 1 Study
- Proof-of-Concept Trial of CERC-501 Augmentation of Antidepressant Therapy in Treatment-Resistant Depression
In development for (14)
- Alcohol dependence Phase 2
- Anxiety Phase 1
- Bipolar disorder Phase 2
- Depressive disorder Phase 2
- Dysthymic disorder Phase 2
- Generalized anxiety disorder Phase 2
- Major depressive disorder Phase 3
- Mood disorder Phase 1
- Nicotine dependence Phase 2
- Obsessive-compulsive disorder Phase 2
- Panic disorder Phase 2
- Post-traumatic stress disorder Phase 2
- Social phobia Phase 2
- Specific phobia Phase 2