Compound Detail
CHEMBL500
PINDOLOL 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL500 |
| Name | PINDOLOL |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | JZQKKSLKJUAGIC-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
15
Targets
39
Activities
4
Assay Types
20
PK Parameters
20
Publications
22
Known Names
3
Indications
2
Mechanisms
Molecular Properties
248.3
MW (Da)
1.91
ALogP
3
HBA
3
HBD
57.3
PSA (Ų)
0.73
QED
0
Ro5 Violations
6
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1982 |
| Availability | Prescription |
| Chirality | Racemic |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Beta-1 adrenergic receptor partial agonist | PARTIAL AGONIST | Beta-1 adrenergic receptor | ✓ | ✓ |
| Beta-2 adrenergic receptor partial agonist | PARTIAL AGONIST | Beta-2 adrenergic receptor | ✓ | ✓ |
Indications
Cardiovascular Diseases Depressive Disorder Depressive Disorder, Major
ATC Classification
C07AA03
pindolol
Level 1: CARDIOVASCULAR SYSTEM
Level 2: BETA BLOCKING AGENTS
Activity Summary
Ki 27 meas. best 9.49
Kd 6 meas. best 9.27
IC50 5 meas. best 9.26
EC50 1 meas. best 7.57
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Beta-2 adrenergic receptor CHEMBL210 | Ki | 9.49 | 9.155 | 0.3 | 4 |
| Beta-1 adrenergic receptor CHEMBL213 | Ki | 9.28 | 9.275 | 0.5 | 2 |
| Beta-2 adrenergic receptor CHEMBL210 | Kd | 9.27 | 9.225 | 0.5 | 2 |
| Beta-2 adrenergic receptor CHEMBL210 | IC50 | 9.26 | 8.96 | 0.5 | 2 |
| Beta-1 adrenergic receptor CHEMBL213 | IC50 | 9.04 | 9.04 | 0.9 | 1 |
| Unchecked CHEMBL612545 | Ki | 9.0 | 9.0 | 1.0 | 2 |
| Beta-1 adrenergic receptor CHEMBL213 | Kd | 8.62 | 8.6 | 2.4 | 2 |
| 5-hydroxytryptamine receptor 1A CHEMBL273 | Ki | 7.7 | 7.6433 | 20.0 | 3 |
| 5-hydroxytryptamine receptor 1A CHEMBL214 | Ki | 7.65 | 7.226 | 22.4 | 5 |
| 5-hydroxytryptamine receptor 1A CHEMBL214 | EC50 | 7.57 | 7.57 | 27.0 | 1 |
| 5-hydroxytryptamine receptor 1A CHEMBL273 | IC50 | 7.32 | 7.32 | 48.0 | 1 |
| 5-hydroxytryptamine receptor 1A CHEMBL214 | Kd | 7.2 | 7.2 | 63.1 | 1 |
| Beta-3 adrenergic receptor CHEMBL246 | Ki | 7.18 | 7.18 | 66.0 | 1 |
| 5-hydroxytryptamine receptor 1B CHEMBL3459 | Ki | 7.1 | 7.1 | 80.0 | 1 |
| Beta-3 adrenergic receptor CHEMBL246 | IC50 | 7.06 | 7.06 | 88.0 | 1 |
| Serotonin 1 (5-HT1) receptor CHEMBL2095159 | Ki | 7.0 | 7.0 | 100.0 | 1 |
| Beta-3 adrenergic receptor CHEMBL246 | Kd | 6.78 | 6.78 | 166.0 | 1 |
| D(3) dopamine receptor CHEMBL234 | Ki | 6.0 | 6.0 | 994.5 | 1 |
| D(4) dopamine receptor CHEMBL219 | Ki | 5.78 | 5.78 | 1661.9 | 1 |
| 5-hydroxytryptamine receptor 1B CHEMBL1898 | Ki | 5.58 | 5.58 | 2600.0 | 1 |
| Sigma intracellular receptor 2 CHEMBL4105907 | Ki | 5.48 | 5.48 | 3315.1 | 1 |
| 5-hydroxytryptamine receptor 5A CHEMBL3426 | Ki | 5.15 | 5.15 | 7048.6 | 1 |
| Serotonin 2 (5-HT2) receptor CHEMBL2093870 | Ki | 4.53 | 4.53 | 29500.0 | 1 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | Ki | 4.27 | 4.27 | 54000.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 4.2 | mL.min-1.kg-1 | Homo sapiens |
| CL | 7.7 | mL.min-1.kg-1 | Homo sapiens |
| CL | 3.8 | mL.min-1.kg-1 | Homo sapiens |
| CL | 7.7 | mL.min-1.kg-1 | Homo sapiens |
| CL | 7.7 | mL.min-1.kg-1 | Homo sapiens |
| CL | 7.59 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| CL | 150.0 | uL.min-1.(10^6cells)-1 | Rattus norvegicus |
| F | 79.0 | % | Homo sapiens |
| F | 92.0 | % | Homo sapiens |
| Fu | 0.58 | - | Homo sapiens |
| Fu | 0.58 | - | Homo sapiens |
| Fu | 0.58 | - | Homo sapiens |
| Fu | 0.43 | - | Rattus norvegicus |
| Fu | 0.4 | - | Rattus norvegicus |
| MRT | 2.6 | hr | Homo sapiens |
| T1/2 | 2.2 | hr | Homo sapiens |
| T1/2 | 3.0 | hr | Rattus norvegicus |
| Tmax | 1.0 | hr | Homo sapiens |
| Vd | 7.2 | L.kg-1 | Rattus norvegicus |
| Vd | 2.0 | L.kg-1 | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine