Compound Detail
CHEMBL723
CARVEDILOL 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL723 |
| Name | CARVEDILOL |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | OGHNVEJMJSYVRP-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
45
Targets
103
Activities
4
Assay Types
20
PK Parameters
20
Publications
24
Known Names
20
Indications
2
Mechanisms
Molecular Properties
406.5
MW (Da)
3.74
ALogP
5
HBA
3
HBD
75.7
PSA (Ų)
0.35
QED
0
Ro5 Violations
10
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1995 |
| Availability | Prescription |
| Chirality | Racemic |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Adrenergic receptor beta antagonist | ANTAGONIST | Adrenergic receptor beta | ✓ | ✓ |
| Adrenergic receptor alpha-1 antagonist | ANTAGONIST | Adrenergic receptor alpha-1 | ✓ | ✓ |
Indications
Cardiovascular Diseases Heart Failure Heart Failure Hypertension Myocardial Infarction Ventricular Dysfunction, Left Atherosclerosis Atrial Fibrillation Coronary Disease Diabetes Mellitus, Type 2 Essential Hypertension Hematologic Neoplasms Hypercholesterolemia Hypertension, Portal Hypertrophy, Left Ventricular Kidney Failure, Chronic Leukemia, Lymphoid Leukemia, Myeloid, Acute Lymphoma Multiple Myeloma
ATC Classification
C07AG02
carvedilol
Level 1: CARDIOVASCULAR SYSTEM
Level 2: BETA BLOCKING AGENTS
Activity Summary
IC50 58 meas. best 9.75
Ki 35 meas. best 9.99
EC50 5 meas. best 5.64
Kd 5 meas. best 9.71
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Beta-1 adrenergic receptor CHEMBL213 | Ki | 9.99 | 9.99 | 0.1 | 1 |
| Beta-2 adrenergic receptor CHEMBL210 | Ki | 9.78 | 9.75 | 0.2 | 2 |
| Beta-1 adrenergic receptor CHEMBL213 | IC50 | 9.75 | 9.75 | 0.2 | 1 |
| Beta-2 adrenergic receptor CHEMBL210 | Kd | 9.71 | 9.71 | 0.2 | 1 |
| Beta-2 adrenergic receptor CHEMBL210 | IC50 | 9.62 | 9.62 | 0.2 | 1 |
| Unchecked CHEMBL612545 | Ki | 9.09 | 6.808 | 0.8 | 5 |
| Beta-1 adrenergic receptor CHEMBL3252 | Ki | 9.09 | 9.09 | 0.8 | 1 |
| Alpha-1D adrenergic receptor CHEMBL223 | Ki | 9.05 | 9.05 | 0.9 | 1 |
| Alpha-1D adrenergic receptor CHEMBL223 | IC50 | 8.75 | 8.75 | 1.8 | 1 |
| Alpha-1B adrenergic receptor CHEMBL315 | Ki | 8.71 | 8.71 | 2.0 | 1 |
| Adrenergic receptor alpha-1 CHEMBL1907610 | Ki | 8.66 | 8.66 | 2.2 | 2 |
| Beta-3 adrenergic receptor CHEMBL246 | Ki | 8.51 | 8.51 | 3.1 | 1 |
| Alpha-1A adrenergic receptor CHEMBL319 | Ki | 8.5 | 8.5 | 3.2 | 1 |
| 5-hydroxytryptamine receptor 1A CHEMBL273 | Ki | 8.5 | 8.49 | 3.2 | 2 |
| Adrenergic receptor alpha-2 CHEMBL2093864 | Ki | 8.47 | 8.47 | 3.4 | 2 |
| Alpha-1B adrenergic receptor CHEMBL315 | IC50 | 8.45 | 8.45 | 3.6 | 1 |
| Beta-3 adrenergic receptor CHEMBL246 | IC50 | 8.38 | 8.38 | 4.2 | 1 |
| 5-hydroxytryptamine receptor 1A CHEMBL273 | IC50 | 8.23 | 8.23 | 5.8 | 1 |
| Alpha-1A adrenergic receptor CHEMBL319 | IC50 | 8.11 | 8.11 | 7.8 | 1 |
| Alpha-2C adrenergic receptor CHEMBL1916 | Ki | 7.89 | 7.89 | 13.0 | 1 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | Ki | 7.82 | 7.82 | 15.0 | 1 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | IC50 | 7.64 | 7.64 | 23.0 | 1 |
| Alpha-2A adrenergic receptor CHEMBL1867 | Ki | 7.4 | 7.4 | 40.0 | 1 |
| Alpha-2B adrenergic receptor CHEMBL1942 | Ki | 7.37 | 7.37 | 43.0 | 1 |
| D(2) dopamine receptor CHEMBL217 | Ki | 7.31 | 7.31 | 49.0 | 1 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | Ki | 7.22 | 7.22 | 60.0 | 1 |
| Alpha-2C adrenergic receptor CHEMBL1916 | IC50 | 7.05 | 7.05 | 90.0 | 1 |
| Alpha-2B adrenergic receptor CHEMBL1942 | IC50 | 7.03 | 7.03 | 94.0 | 1 |
| Unchecked CHEMBL612545 | Kd | 7.0 | 5.93 | 100.0 | 4 |
| Alpha-2A adrenergic receptor CHEMBL1867 | IC50 | 6.97 | 6.97 | 106.0 | 1 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | IC50 | 6.94 | 6.94 | 115.0 | 1 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | Ki | 6.93 | 6.93 | 117.0 | 1 |
| Sodium-dependent serotonin transporter CHEMBL228 | Ki | 6.93 | 6.93 | 118.0 | 1 |
| D(2) dopamine receptor CHEMBL217 | IC50 | 6.84 | 6.84 | 146.0 | 1 |
| 5-hydroxytryptamine receptor 4 CHEMBL5017 | Ki | 6.74 | 6.74 | 181.0 | 1 |
| D(3) dopamine receptor CHEMBL234 | Ki | 6.71 | 6.71 | 196.0 | 1 |
| Sodium-dependent serotonin transporter CHEMBL228 | IC50 | 6.66 | 6.66 | 221.0 | 1 |
| Unchecked CHEMBL612545 | IC50 | 6.51 | 5.7111 | 306.0 | 9 |
| Voltage-gated inwardly rectifying potassium channel KCNH2 CHEMBL240 | IC50 | 6.46 | 5.28 | 350.0 | 6 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | IC50 | 6.39 | 6.39 | 410.0 | 1 |
| Sodium-dependent noradrenaline transporter CHEMBL222 | IC50 | 6.27 | 6.27 | 538.0 | 1 |
| Sodium-dependent noradrenaline transporter CHEMBL222 | Ki | 6.27 | 6.27 | 533.0 | 1 |
| D(3) dopamine receptor CHEMBL234 | IC50 | 6.24 | 6.24 | 577.0 | 1 |
| 5-hydroxytryptamine receptor 1B CHEMBL3459 | Ki | 6.23 | 6.23 | 589.0 | 1 |
| Sodium-dependent dopamine transporter CHEMBL238 | Ki | 6.17 | 6.17 | 671.0 | 1 |
| 5-hydroxytryptamine receptor 6 CHEMBL3371 | Ki | 6.15 | 6.15 | 705.0 | 1 |
| D(1A) dopamine receptor CHEMBL2056 | Ki | 6.13 | 6.13 | 749.0 | 1 |
| Sodium-dependent dopamine transporter CHEMBL238 | IC50 | 6.07 | 6.07 | 845.0 | 1 |
| Cytochrome P450 1B1 CHEMBL4878 | IC50 | 5.96 | 5.96 | 1100.0 | 1 |
| 5-hydroxytryptamine receptor 4 CHEMBL5017 | IC50 | 5.96 | 5.96 | 1088.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 235.0 | mL.min-1.g-1 | Homo sapiens |
| CL | 8.7 | mL.min-1.kg-1 | Homo sapiens |
| CL | 7.8 | mL.min-1.kg-1 | Homo sapiens |
| CL | 7.7 | mL.min-1.kg-1 | Homo sapiens |
| CL | 7.8 | mL.min-1.kg-1 | Homo sapiens |
| CL | 7.8 | mL.min-1.kg-1 | Homo sapiens |
| CL | 26.3 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| CL | 41.69 | mL.min-1.g-1 | Homo sapiens |
| CL | 500.0 | mL/min | Homo sapiens |
| F | 49.0 | % | Homo sapiens |
| F | 25.0 | % | Homo sapiens |
| Fu | 0.02 | - | Homo sapiens |
| Fu | 0.02 | - | Homo sapiens |
| MRT | 2.8 | hr | Homo sapiens |
| T1/2 | 2.4 | hr | Homo sapiens |
| T1/2 | 5.0 | hr | Homo sapiens |
| T1/2 | 7.0 | hr | Homo sapiens |
| T1/2 | 7.0 | hr | Homo sapiens |
| T1/2 | 7.0 | hr | Rattus norvegicus |
| Vss | 115.0 | L | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine