Compound Detail
CHEMBL1101
BIPERIDEN 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL1101 |
| Name | BIPERIDEN |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | YSXKPIUOCJLQIE-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
5
Targets
5
Activities
1
Assay Types
11
PK Parameters
20
Publications
7
Known Names
6
Indications
Molecular Properties
311.5
MW (Da)
3.96
ALogP
2
HBA
1
HBD
23.5
PSA (Ų)
0.83
QED
0
Ro5 Violations
5
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1959 |
| Availability | Discontinued |
| Chirality | Racemic |
Indications
Parkinson Disease Anxiety Cocaine-Related Disorders Dementia Depressive Disorder Schizophrenia
ATC Classification
N04AA02
biperiden
Level 1: NERVOUS SYSTEM
Level 2: ANTI-PARKINSON DRUGS
Activity Summary
Ki 5 meas. best 8.63
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor M1 CHEMBL216 | Ki | 8.63 | 8.63 | 2.4 | 1 |
| Muscarinic acetylcholine receptor M3 CHEMBL245 | Ki | 8.22 | 8.22 | 6.0 | 1 |
| Unchecked CHEMBL612545 | Ki | 7.98 | 7.98 | 10.5 | 1 |
| Muscarinic acetylcholine receptor M2 CHEMBL211 | Ki | 7.86 | 7.86 | 13.7 | 1 |
| Muscarinic acetylcholine receptor M4 CHEMBL1821 | Ki | 7.49 | 7.49 | 32.1 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 12.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 12.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 68.0 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 12.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 15.3 | mL.min-1.kg-1 | Homo sapiens |
| CL | 21.9 | mL.min-1.kg-1 | Macaca |
| CL | 27.0 | mL.min-1.kg-1 | Canis lupus familiaris |
| Fu | 0.097 | - | Homo sapiens |
| Fu | 0.097 | - | Homo sapiens |
| MRT | 17.0 | hr | Homo sapiens |
| T1/2 | 24.0 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor M1 | Ki | = | 2.36 | nM | 8.63 | Displacement of [3H] N-methylscopolamine from human muscarinic M1 receptor expre... | 23523385 |
| Muscarinic acetylcholine receptor M3 | Ki | = | 5.95 | nM | 8.22 | Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expre... | 23523385 |
| Unchecked | Ki | = | 10.5 | nM | 7.98 | Displacement of [3H] N-methylscopolamine from muscarinic acetylcholine receptor ... | 23523385 |
| Muscarinic acetylcholine receptor M2 | Ki | = | 13.7 | nM | 7.86 | Displacement of [3H] N-methylscopolamine from human muscarinic M2 receptor expre... | 23523385 |
| Muscarinic acetylcholine receptor M4 | Ki | = | 32.1 | nM | 7.49 | Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expre... | 23523385 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 31158845 | 10.1038/s41586-019-1291-3 | ADMET | 69 |
| - | 10.5281/zenodo.13943903 | ADMET | 60 |
| 22194678 | 10.1371/journal.pcbi.1002310 | Hepatotoxicity | 14 |
| 20070106 | 10.1021/jm901371v | Homo sapiens | 8 |
| 16621936 | 10.1124/dmd.105.006619 | ADMET | 8 |
| 18426954 | 10.1124/dmd.108.020479 | ADMET | 4 |
| 37468498 | 10.1038/s41467-023-40064-9 | Muscarinic acetylcholine receptor M1 | 4 |
| 37468498 | 10.1038/s41467-023-40064-9 | Nuclear receptor subfamily 1 group I member 2 | 3 |
| 12438524 | 10.1124/jpet.102.039255 | ATP-dependent translocase ABCB1 | 2 |
| 26948801 | 10.1016/j.drudis.2016.02.015 | Homo sapiens | 2 |
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Progesterone receptor | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Peroxisome proliferator-activated receptor gamma | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Muscarinic acetylcholine receptor M2 | 2 |
| 23523385 | 10.1016/j.bmc.2013.01.072 | Muscarinic acetylcholine receptor M1 and M3 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Alpha-1A adrenergic receptor | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 2A | 2 |
| 2579237 | 10.1021/jm00381a019 | Sodium channel alpha subunits; brain (Types I, II, III) | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 2B | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Cannabinoid receptor 1 | 2 |
Data from ChEMBL 36 via Core Engine