Compound Detail
CHEMBL3544974
ASENAPINE MALEATE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL3544974 |
| Name | ASENAPINE MALEATE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | GMDCDXMAFMEDAG-BTJKTKAUSA-N |
| Therapeutic | ✓ Yes |
| Parent Compound | CHEMBL3187365 |
| Active Moiety | CHEMBL3187365 |
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
7
Publications
6
Known Names
6
Indications
2
Mechanisms
Molecular Properties
285.8
MW (Da)
4.26
ALogP
2
HBA
0
HBD
12.5
PSA (Ų)
0.72
QED
0
Ro5 Violations
0
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2009 |
| Availability | Prescription |
| Chirality | Racemic |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Dopamine D2 receptor antagonist | ANTAGONIST | D(2) dopamine receptor | ✓ | ✓ |
| Serotonin 2a (5-HT2a) receptor antagonist | ANTAGONIST | 5-hydroxytryptamine receptor 2A | ✓ | ✓ |
Indications
Bipolar Disorder Bipolar Disorder Schizophrenia Psychotic Disorders Psychotic Disorders Stuttering
Drug Warnings
Black Box Warning
General Warning
Activity Summary
Ki 2 meas. best 8.24
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Histamine H2 receptor CHEMBL1941 | Ki | 8.24 | 8.24 | 5.7 | 2 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Histamine H2 receptor | Ki | = | 5.754 | nM | 8.24 | Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin) | 24365159 |
| Histamine H2 receptor | Ki | = | 5.7 | nM | 8.24 | Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin) | 24365159 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 24365159 | 10.1016/j.bmcl.2013.12.024 | Histamine H2 receptor | 2 |
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 2 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
| 12954186 | 10.1016/s0378-5173(03)00372-7 | ATP-dependent translocase ABCB1 | 1 |
| - | 10.1101/2020.04.03.023846 | SARS-CoV-2 | 1 |
| - | 10.21203/rs.3.rs-23951/v1 | SARS-CoV-2 | 1 |
| - | 10.6019/CHEMBL4495564 | Replicase polyprotein 1ab | 1 |
Data from ChEMBL 36 via Core Engine