Compound Detail
CHEMBL1201023
ORPHENADRINE HYDROCHLORIDE 💊 Approved Drug
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💊 Approved Drug
1
Targets
5
Activities
1
Assay Types
0
PK Parameters
10
Publications
6
Known Names
1
Indications
4
Mechanisms
Molecular Properties
269.4
MW (Da)
3.66
ALogP
2
HBA
0
HBD
12.5
PSA (Ų)
0.79
QED
0
Ro5 Violations
6
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1957 |
| Availability | Discontinued |
| Chirality | Racemic |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Histamine H1 receptor antagonist | ANTAGONIST | Histamine H1 receptor | ✓ | ✓ |
| Norepinephrine transporter inhibitor | INHIBITOR | Sodium-dependent noradrenaline transporter | ✓ | ✓ |
| Glutamate [NMDA] receptor antagonist | ANTAGONIST | Glutamate [NMDA] receptor | ✓ | ✓ |
| Sodium channel alpha subunit blocker | BLOCKER | Sodium channel alpha subunit | ✓ | ✓ |
Indications
Parkinson Disease
ATC Classification
N04AB02
orphenadrine (chloride)
Level 1: NERVOUS SYSTEM
Level 2: ANTI-PARKINSON DRUGS
Activity Summary
IC50 5 meas. best 6.2
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Plasmodium falciparum CHEMBL364 | IC50 | 6.2 | 5.62 | 631.0 | 5 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Plasmodium falciparum | IC50 | = | 630.96 | nM | 6.2 | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR gr... | 19734910 |
| Plasmodium falciparum | IC50 | = | 1258.93 | nM | 5.9 | Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR g... | 19734910 |
| Plasmodium falciparum | IC50 | = | 2511.89 | nM | 5.6 | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR g... | 19734910 |
| Plasmodium falciparum | IC50 | = | 3981.07 | nM | 5.4 | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR g... | 19734910 |
| Plasmodium falciparum | IC50 | = | 10000.0 | nM | 5.0 | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR g... | 19734910 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 19734910 | 10.1038/nchembio.215 | Plasmodium falciparum | 5 |
| 17417631 | 10.1038/nchembio873 | Unchecked | 1 |
| - | 10.1101/2020.04.03.023846 | SARS-CoV-2 | 1 |
| - | 10.6019/CHEMBL4513141 | Candida albicans | 1 |
| - | 10.6019/CHEMBL4513141 | Cryptococcus neoformans | 1 |
| - | 10.6019/CHEMBL4513141 | Escherichia coli | 1 |
| - | 10.6019/CHEMBL4513141 | Klebsiella pneumoniae | 1 |
| - | 10.6019/CHEMBL4513141 | Pseudomonas aeruginosa | 1 |
| - | 10.6019/CHEMBL4513141 | Acinetobacter baumannii | 1 |
| - | 10.6019/CHEMBL4513141 | Staphylococcus aureus | 1 |
Data from ChEMBL 36 via Core Engine