Molecule Details
InChIKeyKPWSJANDNDDRMB-QAQDUYKDSA-N
Canonical SMILESCN(C)C(=O)N[C@H]1CC[C@H](CCN2CCN(c3cccc(Cl)c3Cl)CC2)CC1
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)17
Pfam Stratification Cross-Family
Avg pChEMBL7.37
SourceChEMBL;BindingDB
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB06016
Drug NameCariprazine
CAS Number839712-12-8
Groups approved investigational
ATC Codes N05AX15
DescriptionCariprazine is an atypical antipsychotic agent and a piperazine derivative that was first developed in Hungary.[A247100] It works as a partial agonist at central dopamine D2, dopamine D3, and serotonin 5-HT<sub>1A</sub> receptors and as an antagonist at serotonin 5-HT<sub>2A</sub> receptors.[L40198]...

Categories: Agents that produce hypertension Antidepressive Agents Antipsychotic Agents Antipsychotic Agents (Second Generation [Atypical]) Central Nervous System Agents Central Nervous System Depressants Chlorobenzenes Cyclohexanes Cytochrome P-450 CYP1A2 Inhibitors Cytochrome P-450 CYP1A2 Inhibitors (weak) Cytochrome P-450 CYP2C19 Inhibitors Cytochrome P-450 CYP2C19 Inhibitors (weak) Cytochrome P-450 CYP2C9 Inhibitors Cytochrome P-450 CYP2C9 Inhibitors (weak) Cytochrome P-450 CYP2D6 Inhibitors Cytochrome P-450 CYP2D6 Inhibitors (weak) Cytochrome P-450 CYP2D6 Substrates Cytochrome P-450 CYP2E1 Inhibitors Cytochrome P-450 CYP2E1 Inhibitors (weak) Cytochrome P-450 CYP3A Inducers Cytochrome P-450 CYP3A Inhibitors Cytochrome P-450 CYP3A Substrates Cytochrome P-450 CYP3A4 Inducers Cytochrome P-450 CYP3A4 Inducers (strength unknown) Cytochrome P-450 CYP3A4 Inhibitors Cytochrome P-450 CYP3A4 Inhibitors (weak) Cytochrome P-450 CYP3A4 Substrates Cytochrome P-450 CYP3A5 Inducers Cytochrome P-450 CYP3A5 Inducers (strength unknown) Cytochrome P-450 Enzyme Inducers Cytochrome P-450 Enzyme Inhibitors Cytochrome P-450 Substrates Dopamine Agonists Dopamine D2/D3 receptor modulators Histamine Antagonists Histamine H1 Antagonists Nervous System Neurotoxic agents P-glycoprotein inhibitors Piperazines Psycholeptics Psychotropic Drugs Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome Serotonin 5-HT1 Receptor Agonists Serotonin 5-HT2 Receptor Antagonists Serotonin 5-HT2A Receptor Antagonists Serotonin 5-HT2C Receptor Antagonists Serotonin Agents Serotonin Receptor Agonists Serotonin Receptor Antagonists Tranquilizing Agents
Cross-references: BindingDB: 707646 ChEBI: 90933 CHEMBL2028019 ChemSpider: 25999972 Drugs Product Database (DPD): 23719 D09997 PDB: 7RU PubChem:11154555 PubChem:310264859 RxCUI: 1667655 Wikipedia: Cariprazine ZINC: ZINC000100907004
Target Activities (17)
Target Gene Organism Category Pfam pChEMBL Type Source
P41595 HTR2B Homo sapiens Human PF00001 9.8 Ki ChEMBL
P35462 DRD3 Homo sapiens Human PF00001 9.6 Ki ChEMBL;BindingDB
P14416 DRD2 Homo sapiens Human PF00001 9.1 Ki ChEMBL;BindingDB
P08908 HTR1A Homo sapiens Human PF00001 8.5 Ki ChEMBL
P35367 HRH1 Homo sapiens Human PF00001 7.7 Ki ChEMBL
P28223 HTR2A Homo sapiens Human PF00001 7.6 Ki ChEMBL;BindingDB
P28221 HTR1D Homo sapiens Human PF00001 7.1 Ki ChEMBL
P34969 HTR7 Homo sapiens Human PF00001 7.0 Ki ChEMBL
P28222 HTR1B Homo sapiens Human PF00001 6.9 Ki ChEMBL
P28335 HTR2C Homo sapiens Human PF00001 6.7 Ki ChEMBL
P08588 ADRB1 Homo sapiens Human PF00001 6.7 Ki ChEMBL
P18825 ADRA2C Homo sapiens Human PF00001 6.6 Ki ChEMBL
P35348 ADRA1A Homo sapiens Human PF00001 6.6 Ki ChEMBL
P21917 DRD4 Homo sapiens Human PF00001 6.5 Ki ChEMBL
P25100 ADRA1D Homo sapiens Human PF00001 6.5 Ki ChEMBL
Q5BJF2 TMEM97 Homo sapiens Human PF05241 6.3 Ki ChEMBL
P08173 CHRM4 Homo sapiens Human PF00001 6.1 Ki ChEMBL
DrugBank Target Actions (19)
Target Gene Target Name Action Type
P08684 CYP3A4 Cytochrome P450 3A4 inducer enzymes
P20815 CYP3A5 Cytochrome P450 3A5 inducer enzymes
P05177 CYP1A2 Cytochrome P450 1A2 inhibitor enzymes
P05181 CYP2E1 Cytochrome P450 2E1 inhibitor enzymes
P08684 CYP3A4 Cytochrome P450 3A4 inhibitor enzymes
P10635 CYP2D6 Cytochrome P450 2D6 inhibitor enzymes
P11712 CYP2C9 Cytochrome P450 2C9 inhibitor enzymes
P33261 CYP2C19 Cytochrome P450 2C19 inhibitor enzymes
P08684 CYP3A4 Cytochrome P450 3A4 substrate enzymes
P10635 CYP2D6 Cytochrome P450 2D6 substrate enzymes
P28223 HTR2A 5-hydroxytryptamine receptor 2A antagonist targets
P28335 HTR2C 5-hydroxytryptamine receptor 2C antagonist targets
P35348 ADRA1A Alpha-1A adrenergic receptor antagonist targets
P35367 HRH1 Histamine H1 receptor antagonist targets
P41595 HTR2B 5-hydroxytryptamine receptor 2B antagonist targets
P08908 HTR1A 5-hydroxytryptamine receptor 1A partial agonist targets
P14416 DRD2 D(2) dopamine receptor partial agonist targets
P35462 DRD3 D(3) dopamine receptor partial agonist targets
P08183 ABCB1 ATP-dependent translocase ABCB1 inhibitor transporters