Compound Detail
CHEMBL715
OLANZAPINE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL715 |
| Name | OLANZAPINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | KVWDHTXUZHCGIO-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
55
Targets
297
Activities
4
Assay Types
20
PK Parameters
20
Publications
21
Known Names
20
Indications
3
Mechanisms
Molecular Properties
312.4
MW (Da)
3.44
ALogP
5
HBA
1
HBD
30.9
PSA (Ų)
0.81
QED
0
Ro5 Violations
0
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1996 |
| Availability | Prescription |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Serotonin 2a (5-HT2a) receptor antagonist | ANTAGONIST | 5-hydroxytryptamine receptor 2A | ✓ | ✓ |
| Serotonin 2c (5-HT2c) receptor antagonist | ANTAGONIST | 5-hydroxytryptamine receptor 2C | ✓ | ✓ |
| D2-like dopamine receptor antagonist | ANTAGONIST | D2-like dopamine receptor | ✓ | ✓ |
Indications
Bipolar Disorder Bipolar Disorder Depressive Disorder, Major Mental Disorders Mental Disorders Psychomotor Agitation Psychotic Disorders Psychotic Disorders Schizophrenia Alcoholism Anorexia Anxiety Borderline Personality Disorder Dementia Depressive Disorder Depressive Disorder, Treatment-Resistant Developmental Disabilities Feeding and Eating Disorders Gambling Genital Neoplasms, Female
ATC Classification
N05AH03
olanzapine
Level 1: NERVOUS SYSTEM
Level 2: PSYCHOLEPTICS
Drug Warnings
Black Box Warning
General Warning
Activity Summary
Ki 252 meas. best 9.52
IC50 41 meas. best 8.3
EC50 2 meas. best 8.0
Kd 2 meas. best 10.06
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Histamine H1 receptor CHEMBL231 | Kd | 10.06 | 10.06 | 0.1 | 1 |
| Histamine H1 receptor CHEMBL4701 | Ki | 9.52 | 8.945 | 0.3 | 2 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | Ki | 9.38 | 8.4572 | 0.4 | 25 |
| Histamine H1 receptor CHEMBL231 | Ki | 8.92 | 8.471 | 1.2 | 10 |
| D(2) dopamine receptor CHEMBL217 | Ki | 8.68 | 7.7207 | 2.1 | 30 |
| Muscarinic acetylcholine receptor M1 CHEMBL216 | Ki | 8.68 | 8.0025 | 2.1 | 4 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | Ki | 8.55 | 8.1092 | 2.8 | 12 |
| 5-hydroxytryptamine receptor 2A CHEMBL322 | Ki | 8.4 | 8.3914 | 4.0 | 7 |
| Unchecked CHEMBL612545 | Ki | 8.39 | 7.355 | 4.1 | 4 |
| Dopamine receptor D2 and D3 CHEMBL2111342 | Ki | 8.32 | 7.685 | 4.8 | 2 |
| 5-hydroxytryptamine receptor 6 CHEMBL3371 | Ki | 8.3 | 8.1176 | 5.0 | 21 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | IC50 | 8.3 | 7.875 | 5.0 | 4 |
| Histamine H1 receptor CHEMBL3943 | Ki | 8.2 | 8.2 | 6.3 | 1 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | Ki | 8.2 | 7.8533 | 6.3 | 3 |
| D(2) dopamine receptor CHEMBL339 | Ki | 8.15 | 7.4436 | 7.0 | 14 |
| Adrenergic receptor alpha-1 CHEMBL2094251 | Ki | 8.14 | 7.75 | 7.3 | 5 |
| Mus musculus CHEMBL375 | EC50 | 8.0 | 8.0 | 10.0 | 1 |
| D(2) dopamine receptor CHEMBL217 | IC50 | 8.0 | 7.465 | 10.0 | 2 |
| Serotonin 2 (5-HT2) receptor CHEMBL2095200 | Ki | 8.0 | 8.0 | 10.0 | 1 |
| D(1A) dopamine receptor CHEMBL2056 | Ki | 8.0 | 7.2233 | 10.0 | 9 |
| Muscarinic acetylcholine receptor M5 CHEMBL2035 | Ki | 8.0 | 7.77 | 10.0 | 2 |
| Serotonin 2 (5-HT2) receptor CHEMBL2093870 | Ki | 7.92 | 7.91 | 12.0 | 2 |
| Muscarinic acetylcholine receptor M4 CHEMBL1821 | Ki | 7.9 | 7.1867 | 12.6 | 3 |
| 5-hydroxytryptamine receptor 6 CHEMBL3371 | IC50 | 7.89 | 7.89 | 13.0 | 1 |
| Histamine H1 receptor CHEMBL231 | IC50 | 7.89 | 7.89 | 13.0 | 1 |
| Histamine H1 receptor CHEMBL4701 | IC50 | 7.89 | 7.89 | 13.0 | 1 |
| Adrenergic receptor alpha-1 CHEMBL1907610 | Ki | 7.84 | 7.58 | 14.6 | 4 |
| D(4) dopamine receptor CHEMBL219 | Ki | 7.72 | 7.4888 | 19.0 | 8 |
| D(3) dopamine receptor CHEMBL234 | Ki | 7.7 | 7.3633 | 19.9 | 12 |
| D(1A) dopamine receptor CHEMBL265 | Ki | 7.7 | 7.1867 | 20.0 | 9 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | IC50 | 7.68 | 7.415 | 21.0 | 2 |
| Alpha-1B adrenergic receptor CHEMBL315 | Ki | 7.68 | 7.42 | 21.0 | 2 |
| Muscarinic acetylcholine receptor M1 CHEMBL276 | Ki | 7.66 | 7.66 | 22.0 | 2 |
| Alpha-1A adrenergic receptor CHEMBL319 | Ki | 7.6 | 7.59 | 25.1 | 2 |
| Muscarinic acetylcholine receptor CHEMBL2094109 | Ki | 7.58 | 7.375 | 26.0 | 2 |
| Alpha-1B adrenergic receptor CHEMBL315 | IC50 | 7.43 | 7.43 | 37.0 | 1 |
| D(3) dopamine receptor CHEMBL3138 | Ki | 7.41 | 7.345 | 38.9 | 6 |
| Muscarinic acetylcholine receptor M5 CHEMBL2035 | IC50 | 7.4 | 7.4 | 40.0 | 1 |
| Alpha-1D adrenergic receptor CHEMBL223 | Ki | 7.35 | 7.35 | 45.0 | 1 |
| Serotonin 2 (5-HT2) receptor CHEMBL2093870 | IC50 | 7.33 | 7.33 | 47.0 | 1 |
| D(4) dopamine receptor CHEMBL3361 | Ki | 7.3 | 7.3 | 50.0 | 1 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | IC50 | 7.24 | 7.24 | 57.0 | 1 |
| Alpha-1A adrenergic receptor CHEMBL229 | Ki | 7.22 | 6.8133 | 60.0 | 3 |
| Alpha-1A adrenergic receptor CHEMBL319 | IC50 | 7.19 | 7.19 | 65.0 | 1 |
| D(1A) dopamine receptor CHEMBL2056 | IC50 | 7.14 | 7.14 | 72.0 | 1 |
| Alpha-2C adrenergic receptor CHEMBL1916 | Ki | 7.11 | 7.0667 | 77.0 | 3 |
| D(3) dopamine receptor CHEMBL234 | IC50 | 7.11 | 7.11 | 78.0 | 1 |
| 5-hydroxytryptamine receptor 7 CHEMBL3155 | Ki | 7.1 | 6.592 | 79.4 | 5 |
| Muscarinic acetylcholine receptor M3 CHEMBL245 | Ki | 7.08 | 7.04 | 83.0 | 2 |
| D(1B) dopamine receptor CHEMBL1850 | Ki | 7.05 | 7.025 | 90.0 | 2 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 184.7 | - | Rattus norvegicus |
| AUC | 157.7 | - | Rattus norvegicus |
| AUC | 113.1 | - | Rattus norvegicus |
| AUC | 220.8 | - | Rattus norvegicus |
| AUC | 20.73 | - | Rattus norvegicus |
| AUC | 143.7 | - | Rattus norvegicus |
| AUC | 2.8 | - | Rattus norvegicus |
| AUC | 1825.0 | - | Rattus norvegicus |
| AUC | 128.4 | - | Rattus norvegicus |
| AUC | 288.8 | - | Chlorocebus sabaeus |
| CL | 0.000113 | mL.min-1.g-1 | Homo sapiens |
| CL | 6e-06 | mL.min-1.g-1 | Homo sapiens |
| CL | 0.119 | uL/min | Homo sapiens |
| CL(app) | 25.0 | L/hr | Homo sapiens |
| Excretion | 7.0 | % | Homo sapiens |
| F | 79.0 | % | Homo sapiens |
| Fu | 0.034 | - | Rattus norvegicus |
| T1/2 | 30.0 | hr | Homo sapiens |
| Tmax | 6.0 | hr | Homo sapiens |
| Vd | 1000.0 | L | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine