Compound Detail
CHEMBL1706
NAPHAZOLINE HYDROCHLORIDE 💊 Approved Drug
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💊 Approved Drug
3
Targets
6
Activities
2
Assay Types
0
PK Parameters
20
Publications
17
Known Names
8
Indications
1
Mechanisms
Molecular Properties
210.3
MW (Da)
2.38
ALogP
2
HBA
1
HBD
24.4
PSA (Ų)
0.81
QED
0
Ro5 Violations
2
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1971 |
| Availability | OTC |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Adrenergic receptor alpha agonist | AGONIST | Adrenergic receptor alpha | ✓ | ✓ |
Indications
Common Cold Nasal Obstruction Rhinitis, Allergic, Seasonal Sinusitis Inflammation Influenza, Human Pterygium Respiratory Tract Diseases
Activity Summary
IC50 4 meas. best 5.94
EC50 2 meas. best 7.92
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Adrenergic receptor alpha-1 CHEMBL1907610 | EC50 | 7.92 | 7.92 | 12.0 | 1 |
| Trace amine-associated receptor 1 CHEMBL5857 | EC50 | 6.85 | 6.85 | 140.2 | 1 |
| Trace amine-associated receptor 1 CHEMBL5857 | IC50 | 5.94 | 5.94 | 1154.0 | 1 |
| Plasmodium falciparum CHEMBL364 | IC50 | 5.0 | 5.0 | 10000.0 | 2 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Adrenergic receptor alpha-1 | EC50 | = | 12.0 | nM | 7.92 | Compound was evaluated for Adrenergic activity against Alpha-1 adrenergic recept... | 1347319 |
| Trace amine-associated receptor 1 | EC50 | = | 140.18 | nM | 6.85 | PubChem BioAssay. Fluorescence-based cell-based high throughput dose response as... | - |
| Trace amine-associated receptor 1 | IC50 | = | 1154.0 | nM | 5.94 | PubChem BioAssay. Counterscreen for agonists of the human trace amine associated... | - |
| Plasmodium falciparum | IC50 | = | 10000.0 | nM | 5.0 | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR g... | 19734910 |
| Plasmodium falciparum | IC50 | = | 10000.0 | nM | 5.0 | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR gr... | 19734910 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 1347319 | 10.1021/jm00082a017 | Unchecked | 2 |
| 19734910 | 10.1038/nchembio.215 | Plasmodium falciparum | 2 |
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 2 |
| - | 10.21203/rs.3.rs-23951/v1 | SARS-CoV-2 | 1 |
| - | 10.6019/EOS300033 | SARS-CoV-2 | 1 |
| - | 10.6019/CHEMBL4513141 | Staphylococcus aureus | 1 |
| - | 10.6019/CHEMBL4513141 | Acinetobacter baumannii | 1 |
| - | 10.6019/CHEMBL4513141 | Pseudomonas aeruginosa | 1 |
| - | 10.6019/CHEMBL4513141 | Klebsiella pneumoniae | 1 |
| - | 10.6019/CHEMBL4513141 | Escherichia coli | 1 |
| - | 10.6019/CHEMBL4513141 | Cryptococcus neoformans | 1 |
| - | 10.6019/CHEMBL4513141 | Candida albicans | 1 |
| - | 10.6019/CHEMBL4495564 | Replicase polyprotein 1ab | 1 |
| 1347319 | 10.1021/jm00082a017 | Adrenergic receptor alpha-1 | 1 |
| - | 10.1101/2020.04.03.023846 | SARS-CoV-2 | 1 |
| 23571415 | 10.1124/mol.112.084152 | Solute carrier organic anion transporter family member 1B3 | 1 |
| 23571415 | 10.1124/mol.112.084152 | Solute carrier organic anion transporter family member 1B1 | 1 |
| 23129510 | 10.1002/ps.3378 | TyR1 | 1 |
| 17417631 | 10.1038/nchembio873 | Unchecked | 1 |
| 1347319 | 10.1021/jm00082a017 | Adrenergic receptor alpha-2 | 1 |
Data from ChEMBL 36 via Core Engine