Compound Detail
CHEMBL1201216
DAPIPRAZOLE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL1201216 |
| Name | DAPIPRAZOLE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | RFWZESUMWJKKRN-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
8
Targets
16
Activities
2
Assay Types
0
PK Parameters
20
Publications
2
Known Names
1
Indications
Molecular Properties
325.5
MW (Da)
2.29
ALogP
5
HBA
0
HBD
37.2
PSA (Ų)
0.86
QED
0
Ro5 Violations
4
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1990 |
| Availability | Discontinued |
| Chirality | Achiral |
Indications
Glaucoma
ATC Classification
S01EX02
dapiprazole
Level 1: SENSORY ORGANS
Level 2: OPHTHALMOLOGICALS
Activity Summary
IC50 8 meas. best 8.08
Ki 8 meas. best 8.39
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Alpha-1D adrenergic receptor CHEMBL223 | Ki | 8.39 | 8.39 | 4.1 | 1 |
| Alpha-1D adrenergic receptor CHEMBL223 | IC50 | 8.08 | 8.08 | 8.3 | 1 |
| Alpha-1B adrenergic receptor CHEMBL315 | Ki | 7.52 | 7.52 | 30.0 | 1 |
| Alpha-1A adrenergic receptor CHEMBL319 | Ki | 7.41 | 7.41 | 39.0 | 1 |
| Alpha-1B adrenergic receptor CHEMBL315 | IC50 | 7.26 | 7.26 | 55.0 | 1 |
| Alpha-1A adrenergic receptor CHEMBL319 | IC50 | 7.02 | 7.02 | 95.0 | 1 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | Ki | 6.76 | 6.76 | 173.0 | 1 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | Ki | 6.49 | 6.49 | 327.0 | 1 |
| Alpha-2B adrenergic receptor CHEMBL1942 | Ki | 6.28 | 6.28 | 526.0 | 1 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | IC50 | 6.22 | 6.22 | 606.0 | 1 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | IC50 | 6.2 | 6.2 | 625.0 | 1 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | Ki | 6.17 | 6.17 | 672.0 | 1 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | IC50 | 5.98 | 5.98 | 1056.0 | 1 |
| Alpha-2B adrenergic receptor CHEMBL1942 | IC50 | 5.94 | 5.94 | 1153.0 | 1 |
| 5-hydroxytryptamine receptor 1A CHEMBL273 | Ki | 5.93 | 5.93 | 1177.0 | 1 |
| 5-hydroxytryptamine receptor 1A CHEMBL273 | IC50 | 5.69 | 5.69 | 2060.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 16472241 | 10.2174/1570163043334794 | Hepatotoxicity | 18 |
| 37468498 | 10.1038/s41467-023-40064-9 | Prostaglandin G/H synthase 1 | 2 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Thromboxane A2 receptor | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Alpha-1A adrenergic receptor | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Muscarinic acetylcholine receptor M1 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Alpha-2A adrenergic receptor | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Muscarinic acetylcholine receptor M2 | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Vascular endothelial growth factor receptor 2 | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 1A | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Amine oxidase [flavin-containing] A | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Mu-type opioid receptor | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Sodium-dependent serotonin transporter | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Sodium-dependent noradrenaline transporter | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Acetylcholinesterase | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Estrogen receptor | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Sodium-dependent dopamine transporter | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Voltage-gated inwardly rectifying potassium channel KCNH2 | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | D(1A) dopamine receptor | 1 |
Data from ChEMBL 36 via Core Engine