Compound Detail
CHEMBL493
BROMOCRIPTINE 💊 Approved Drug
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💊 Approved Drug
CC(C)C[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]c(Br)c(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12
Basic Information
| ChEMBL ID | CHEMBL493 |
| Name | BROMOCRIPTINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | OZVBMTJYIDMWIL-AYFBDAFISA-N |
| Therapeutic | ✓ Yes |
36
Targets
80
Activities
4
Assay Types
13
PK Parameters
20
Publications
8
Known Names
9
Indications
Molecular Properties
654.6
MW (Da)
3.19
ALogP
6
HBA
3
HBD
118.2
PSA (Ų)
0.46
QED
1
Ro5 Violations
5
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1978 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Indications
Parkinson Disease Peripartum Cardiomyopathy Diabetes Mellitus, Type 1 Intellectual Disability Obesity Ovarian Hyperstimulation Syndrome Adenomyosis Alzheimer Disease Anorexia Nervosa
ATC Classification
G02CB01
bromocriptine
Level 1: GENITO URINARY SYSTEM AND SEX HORMONES
Level 2: OTHER GYNECOLOGICALS
N04BC01
bromocriptine
Level 1: NERVOUS SYSTEM
Level 2: ANTI-PARKINSON DRUGS
Activity Summary
Ki 37 meas. best 9.7
IC50 28 meas. best 9.22
EC50 11 meas. best 9.3
Kd 4 meas. best 8.4
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| D(3) dopamine receptor CHEMBL234 | Ki | 9.7 | 7.94 | 0.2 | 3 |
| D(2) dopamine receptor CHEMBL217 | EC50 | 9.3 | 9.3 | 0.5 | 1 |
| D(2) dopamine receptor CHEMBL217 | Ki | 9.28 | 8.3567 | 0.5 | 6 |
| D(3) dopamine receptor CHEMBL234 | IC50 | 9.22 | 9.22 | 0.6 | 1 |
| D(2) dopamine receptor CHEMBL217 | IC50 | 8.8 | 8.8 | 1.6 | 1 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | EC50 | 8.75 | 8.75 | 1.8 | 1 |
| Alpha-1B adrenergic receptor CHEMBL315 | Ki | 8.71 | 8.71 | 2.0 | 1 |
| Alpha-1A adrenergic receptor CHEMBL319 | Ki | 8.55 | 8.55 | 2.8 | 1 |
| 5-hydroxytryptamine receptor 1A CHEMBL273 | Ki | 8.49 | 8.49 | 3.2 | 1 |
| Alpha-1B adrenergic receptor CHEMBL315 | IC50 | 8.45 | 8.45 | 3.5 | 1 |
| D(2) dopamine receptor CHEMBL339 | Kd | 8.4 | 8.0925 | 4.0 | 4 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | Ki | 8.28 | 8.28 | 5.3 | 1 |
| Alpha-2A adrenergic receptor CHEMBL1867 | Ki | 8.26 | 7.92 | 5.5 | 2 |
| 5-hydroxytryptamine receptor 1A CHEMBL273 | IC50 | 8.25 | 8.25 | 5.6 | 1 |
| Alpha-1A adrenergic receptor CHEMBL319 | IC50 | 8.16 | 8.16 | 7.0 | 1 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | IC50 | 8.08 | 8.08 | 8.3 | 1 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | Ki | 8.0 | 7.46 | 10.0 | 2 |
| 5-hydroxytryptamine receptor 6 CHEMBL3371 | Ki | 8.0 | 8.0 | 10.0 | 1 |
| Alpha-1D adrenergic receptor CHEMBL223 | Ki | 7.82 | 7.82 | 15.0 | 1 |
| Alpha-2A adrenergic receptor CHEMBL1867 | IC50 | 7.82 | 7.82 | 15.0 | 1 |
| Alpha-2B adrenergic receptor CHEMBL1942 | Ki | 7.8 | 7.8 | 16.0 | 1 |
| Alpha-1A adrenergic receptor CHEMBL229 | Ki | 7.75 | 7.75 | 18.0 | 1 |
| 5-hydroxytryptamine receptor 6 CHEMBL3371 | IC50 | 7.66 | 7.66 | 22.0 | 1 |
| 5-hydroxytryptamine receptor 1A CHEMBL214 | Ki | 7.62 | 7.62 | 24.0 | 2 |
| Dopamine receptor CHEMBL2093868 | IC50 | 7.55 | 7.55 | 27.9 | 2 |
| Alpha-1D adrenergic receptor CHEMBL223 | IC50 | 7.52 | 7.52 | 30.0 | 1 |
| Unchecked CHEMBL612545 | Ki | 7.46 | 6.335 | 35.0 | 2 |
| Alpha-2B adrenergic receptor CHEMBL1942 | IC50 | 7.46 | 7.46 | 35.0 | 1 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | IC50 | 7.44 | 7.44 | 36.0 | 1 |
| 5-hydroxytryptamine receptor 1B CHEMBL3459 | Ki | 7.33 | 7.33 | 47.0 | 1 |
| Unchecked CHEMBL612545 | IC50 | 7.28 | 6.225 | 53.0 | 2 |
| Alpha-2C adrenergic receptor CHEMBL1916 | Ki | 7.12 | 7.12 | 76.0 | 1 |
| 5-hydroxytryptamine receptor 1B CHEMBL3459 | IC50 | 6.99 | 6.99 | 103.0 | 1 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | Ki | 6.56 | 6.56 | 278.0 | 1 |
| D(4) dopamine receptor CHEMBL219 | Ki | 6.43 | 6.43 | 373.0 | 1 |
| Cerebral cortex alpha adrenergic receptor CHEMBL2111420 | IC50 | 6.29 | 6.29 | 514.0 | 1 |
| Adrenergic receptor alpha-2 CHEMBL2093864 | IC50 | 6.29 | 6.29 | 514.0 | 1 |
| Alpha-2C adrenergic receptor CHEMBL1916 | IC50 | 6.28 | 6.28 | 520.0 | 1 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | IC50 | 6.27 | 6.27 | 532.0 | 1 |
| dengue virus type 4 CHEMBL613728 | EC50 | 6.1 | 6.1 | 800.0 | 1 |
| dengue virus type 2 CHEMBL613966 | EC50 | 6.1 | 6.1 | 800.0 | 1 |
| dengue virus type 3 CHEMBL612717 | EC50 | 6.1 | 6.1 | 800.0 | 1 |
| NON-PROTEIN TARGET CHEMBL3879801 | EC50 | 5.92 | 5.76 | 1200.0 | 2 |
| Beta-1 adrenergic receptor CHEMBL213 | Ki | 5.86 | 5.86 | 1386.0 | 1 |
| D(1A) dopamine receptor CHEMBL2056 | Ki | 5.84 | 5.655 | 1444.0 | 2 |
| Androgen receptor CHEMBL3072 | Ki | 5.82 | 5.82 | 1521.0 | 1 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | EC50 | 5.8 | 5.8 | 1584.9 | 1 |
| dengue virus type 1 CHEMBL613360 | EC50 | 5.8 | 5.8 | 1600.0 | 1 |
| Cytochrome P450 3A4 CHEMBL340 | IC50 | 5.7 | 5.61 | 2000.0 | 2 |
| Androgen receptor CHEMBL3072 | IC50 | 5.64 | 5.64 | 2281.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 2.377 | ng.hr.mL-1 | Mus musculus |
| Cmax | 0.711 | nM | Homo sapiens |
| Cmax | 0.000628 | ug.mL-1 | Homo sapiens |
| F | 4.5 | % | Homo sapiens |
| F | 90.0 | % | Mus musculus |
| Fu | 0.002 | - | Homo sapiens |
| Fu | 0.002 | - | Macaca fascicularis |
| Fu | 0.002 | - | Canis lupus familiaris |
| Fu | 0.002 | - | Cavia porcellus |
| Fu | 0.002 | - | Mus musculus |
| Fu | 0.001 | - | Rattus norvegicus |
| Fu | 0.002 | - | Rattus norvegicus |
| T1/2 | 4.85 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine