Compound Detail
CHEMBL86715
PROCYCLIDINE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL86715 |
| Name | PROCYCLIDINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | WYDUSKDSKCASEF-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
3
Targets
3
Activities
2
Assay Types
6
PK Parameters
20
Publications
8
Known Names
1
Indications
Molecular Properties
287.4
MW (Da)
3.94
ALogP
2
HBA
1
HBD
23.5
PSA (Ų)
0.89
QED
0
Ro5 Violations
5
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1955 |
| Availability | Discontinued |
| Chirality | Racemic |
Indications
Parkinson Disease
ATC Classification
N04AA04
procyclidine
Level 1: NERVOUS SYSTEM
Level 2: ANTI-PARKINSON DRUGS
Activity Summary
IC50 2 meas. best 5.17
Ki 1 meas. best 5.77
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Glutamate [NMDA] receptor CHEMBL2094124 | Ki | 5.77 | 5.77 | 1700.0 | 1 |
| Histamine H1 receptor CHEMBL4701 | IC50 | 5.17 | 5.17 | 6760.8 | 1 |
| Histamine H1 receptor CHEMBL231 | IC50 | 4.75 | 4.75 | 17782.8 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 0.8 | mL.min-1.kg-1 | Homo sapiens |
| CL | 0.86 | mL.min-1.kg-1 | Homo sapiens |
| CL | 0.86 | mL.min-1.kg-1 | Homo sapiens |
| F | 79.0 | % | Homo sapiens |
| MRT | 14.0 | hr | Homo sapiens |
| T1/2 | 12.0 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Glutamate [NMDA] receptor | Ki | = | 1700.0 | nM | 5.77 | The compound was tested for its ability to block PCP N-methyl-D-aspartate glutam... | 9464369 |
| Histamine H1 receptor | IC50 | = | 6760.83 | nM | 5.17 | Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat ... | 22793499 |
| Histamine H1 receptor | IC50 | = | 17782.79 | nM | 4.75 | Antagonist activity at H1 receptor in human HeLa cells assessed as inhibition of... | 22793499 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 22194678 | 10.1371/journal.pcbi.1002310 | Hepatotoxicity | 14 |
| 20070106 | 10.1021/jm901371v | Homo sapiens | 8 |
| 18426954 | 10.1124/dmd.108.020479 | ADMET | 4 |
| 37468498 | 10.1038/s41467-023-40064-9 | Muscarinic acetylcholine receptor M2 | 4 |
| 37468498 | 10.1038/s41467-023-40064-9 | Muscarinic acetylcholine receptor M1 | 3 |
| 10891117 | 10.1021/jm0000564 | No relevant target | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Gamma-aminobutyric acid receptor subunit alpha-1 | 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 | Progesterone receptor | 2 |
| 22793499 | 10.1021/jm300671m | Histamine H1 receptor | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Alpha-2A adrenergic receptor | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 2A | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 1A | 2 |
| 10891117 | 10.1021/jm0000564 | ADMET | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 2B | 2 |
| - | 10.6019/CHEMBL3301361 | No relevant target | 1 |
| 23956101 | 10.1093/toxsci/kft176 | Bile salt export pump | 1 |
| 38318365 | 10.1016/j.isci.2024.108907 | Deoxynucleoside triphosphate triphosphohydrolase SAMHD1 | 1 |
Data from ChEMBL 36 via Core Engine