Compound Detail
CHEMBL395110
MEPAZINE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL395110 |
| Name | MEPAZINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | CBHCDHNUZWWAPP-UHFFFAOYSA-N |
20
Targets
47
Activities
2
Assay Types
0
PK Parameters
20
Publications
17
Known Names
Molecular Properties
310.5
MW (Da)
4.63
ALogP
3
HBA
0
HBD
6.5
PSA (Ų)
0.80
QED
0
Ro5 Violations
2
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Availability | Withdrawn |
| Chirality | Racemic |
Activity Summary
IC50 26 meas. best 7.57
Ki 21 meas. best 8.51
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Histamine H1 receptor CHEMBL231 | Ki | 8.51 | 8.51 | 3.1 | 1 |
| Muscarinic acetylcholine receptor M4 CHEMBL1821 | Ki | 7.72 | 7.72 | 19.0 | 1 |
| Muscarinic acetylcholine receptor M1 CHEMBL216 | Ki | 7.72 | 7.72 | 19.0 | 1 |
| Histamine H1 receptor CHEMBL231 | IC50 | 7.57 | 7.57 | 27.0 | 1 |
| Muscarinic acetylcholine receptor M5 CHEMBL2035 | Ki | 7.55 | 7.55 | 28.0 | 1 |
| Alpha-1B adrenergic receptor CHEMBL315 | Ki | 7.47 | 7.47 | 34.0 | 1 |
| Muscarinic acetylcholine receptor M3 CHEMBL245 | Ki | 7.4 | 7.4 | 40.0 | 1 |
| Muscarinic acetylcholine receptor M5 CHEMBL2035 | IC50 | 7.4 | 7.4 | 40.0 | 1 |
| Alpha-1A adrenergic receptor CHEMBL319 | Ki | 7.24 | 7.24 | 58.0 | 1 |
| Alpha-1B adrenergic receptor CHEMBL315 | IC50 | 7.21 | 7.21 | 61.0 | 1 |
| Alpha-1D adrenergic receptor CHEMBL223 | Ki | 7.17 | 7.17 | 67.0 | 1 |
| Sigma non-opioid intracellular receptor 1 CHEMBL287 | Ki | 7.12 | 7.12 | 76.0 | 1 |
| Muscarinic acetylcholine receptor M1 CHEMBL216 | IC50 | 7.1 | 7.1 | 79.0 | 1 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | Ki | 6.96 | 6.96 | 110.0 | 1 |
| Alpha-1D adrenergic receptor CHEMBL223 | IC50 | 6.86 | 6.86 | 137.0 | 1 |
| Muscarinic acetylcholine receptor M4 CHEMBL1821 | IC50 | 6.86 | 6.86 | 137.0 | 1 |
| Alpha-1A adrenergic receptor CHEMBL319 | IC50 | 6.84 | 6.84 | 144.0 | 1 |
| Sigma non-opioid intracellular receptor 1 CHEMBL287 | IC50 | 6.75 | 6.75 | 180.0 | 1 |
| Alpha-2B adrenergic receptor CHEMBL1942 | Ki | 6.74 | 6.74 | 181.0 | 1 |
| Muscarinic acetylcholine receptor M3 CHEMBL245 | IC50 | 6.72 | 6.72 | 191.0 | 1 |
| Muscarinic acetylcholine receptor M2 CHEMBL211 | Ki | 6.7 | 6.7 | 201.0 | 1 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | Ki | 6.59 | 6.59 | 259.0 | 1 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | Ki | 6.49 | 6.49 | 327.0 | 1 |
| 5-hydroxytryptamine receptor 2A CHEMBL224 | IC50 | 6.42 | 6.42 | 385.0 | 1 |
| Unchecked CHEMBL612545 | Ki | 6.41 | 5.9567 | 388.0 | 3 |
| Alpha-2B adrenergic receptor CHEMBL1942 | IC50 | 6.4 | 6.4 | 397.0 | 1 |
| Mucosa-associated lymphoid tissue lymphoma translocation protein 1 CHEMBL3632452 | IC50 | 6.38 | 6.155 | 420.0 | 4 |
| 5-hydroxytryptamine receptor 2C CHEMBL225 | IC50 | 6.3 | 6.3 | 495.0 | 1 |
| 5-hydroxytryptamine receptor 2B CHEMBL1833 | IC50 | 6.29 | 6.29 | 514.0 | 1 |
| Alpha-2A adrenergic receptor CHEMBL1867 | Ki | 6.26 | 6.26 | 546.0 | 1 |
| Muscarinic acetylcholine receptor M2 CHEMBL211 | IC50 | 6.25 | 6.25 | 565.0 | 1 |
| Unchecked CHEMBL612545 | IC50 | 6.2 | 5.92 | 631.0 | 4 |
| D(3) dopamine receptor CHEMBL234 | Ki | 6.17 | 6.17 | 681.0 | 1 |
| 5-hydroxytryptamine receptor 6 CHEMBL3371 | Ki | 6.07 | 6.07 | 853.0 | 1 |
| Alpha-2A adrenergic receptor CHEMBL1867 | IC50 | 5.84 | 5.84 | 1456.0 | 1 |
| 5-hydroxytryptamine receptor 6 CHEMBL3371 | IC50 | 5.74 | 5.74 | 1837.0 | 1 |
| Sodium-dependent noradrenaline transporter CHEMBL222 | Ki | 5.73 | 5.73 | 1861.0 | 1 |
| Sodium-dependent noradrenaline transporter CHEMBL222 | IC50 | 5.73 | 5.73 | 1877.0 | 1 |
| D(3) dopamine receptor CHEMBL234 | IC50 | 5.7 | 5.7 | 2006.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 27085674 | 10.1016/j.bmc.2016.03.035 | Mucosa-associated lymphoid tissue lymphoma translocation protein 1 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Thromboxane A2 receptor | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Prostaglandin G/H synthase 1 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Alpha-1A adrenergic receptor | 2 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
| - | 10.6019/CHEMBL4651402 | SARS-CoV-2 | 2 |
| 26948801 | 10.1016/j.drudis.2016.02.015 | Homo sapiens | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Muscarinic acetylcholine receptor M1 | 2 |
| 21624500 | 10.1016/j.drudis.2011.05.007 | Hepatotoxicity | 1 |
| - | 10.1039/C4MD00030G | Serine/threonine-protein kinase pim-1 | 1 |
| 38349664 | 10.1021/acs.jmedchem.3c02031 | Mucosa-associated lymphoid tissue lymphoma translocation protein 1 | 1 |
| 17407813 | 10.1016/j.bmcl.2007.03.064 | 5-hydroxytryptamine receptor 2C | 1 |
| 17407813 | 10.1016/j.bmcl.2007.03.064 | 5-hydroxytryptamine receptor 2A | 1 |
| 17407813 | 10.1016/j.bmcl.2007.03.064 | 5-hydroxytryptamine receptor 1A | 1 |
| 34181850 | 10.1021/acs.jmedchem.1c00466 | Mucosa-associated lymphoid tissue lymphoma translocation protein 1 | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | D(1A) dopamine receptor | 1 |
| 17407813 | 10.1016/j.bmcl.2007.03.064 | D(3) dopamine receptor | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Sodium-dependent dopamine transporter | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Bile salt export pump | 1 |
| 17407813 | 10.1016/j.bmcl.2007.03.064 | D(2) dopamine receptor | 1 |
Data from ChEMBL 36 via Core Engine