Compound Detail
CHEMBL1305
ANTAZOLINE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL1305 |
| Name | ANTAZOLINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | REYFJDPCWQRWAA-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
2
Targets
5
Activities
2
Assay Types
0
PK Parameters
20
Publications
5
Known Names
2
Indications
Molecular Properties
265.4
MW (Da)
2.69
ALogP
3
HBA
1
HBD
27.6
PSA (Ų)
0.90
QED
0
Ro5 Violations
5
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1994 |
| Availability | Discontinued |
| Chirality | Achiral |
Indications
Hypersensitivity Nasal Obstruction
ATC Classification
R01AC04
antazoline
Level 1: RESPIRATORY SYSTEM
Level 2: NASAL PREPARATIONS
R06AX05
antazoline
Level 1: RESPIRATORY SYSTEM
Level 2: ANTIHISTAMINES FOR SYSTEMIC USE
Activity Summary
Kd 4 meas. best 7.14
IC50 1 meas. best 5.9
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Histamine H1 receptor CHEMBL3943 | Kd | 7.14 | 7.14 | 72.4 | 4 |
| Rattus norvegicus CHEMBL376 | IC50 | 5.9 | 5.9 | 1260.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Histamine H1 receptor | Kd | = | 72.44 | nM | 7.14 | Antagonist potency at histamine H1 receptor in guinea-pig ileum assessed as inhi... | 29681486 |
| Histamine H1 receptor | Kd | = | 72.44 | nM | 7.14 | Antagonist activity at H1 receptor in guinea pig ileum assessed as inhibition of... | 29723785 |
| Histamine H1 receptor | Kd | = | 72.44 | nM | 7.14 | Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inh... | 28797771 |
| Histamine H1 receptor | Kd | = | 72.44 | nM | 7.14 | Antagonist activity at histamine H1 receptor in guinea-pig ileum assessed as inh... | 30792106 |
| Rattus norvegicus | IC50 | = | 1260.0 | nM | 5.9 | Compound was evaluated in vivo for inhibition of Ovalbumin induced rhinitis in a... | 10052971 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| - | 10.5281/zenodo.13943903 | ADMET | 89 |
| 31158845 | 10.1038/s41586-019-1291-3 | ADMET | 60 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 1A | 4 |
| 37468498 | 10.1038/s41467-023-40064-9 | Muscarinic acetylcholine receptor M2 | 4 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 2B | 4 |
| 37468498 | 10.1038/s41467-023-40064-9 | Alpha-2A adrenergic receptor | 4 |
| 37468498 | 10.1038/s41467-023-40064-9 | Prostaglandin G/H synthase 1 | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | Muscarinic acetylcholine receptor M1 | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | Alpha-1A adrenergic receptor | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | D(1A) dopamine receptor | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | Thromboxane A2 receptor | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | Gamma-aminobutyric acid receptor subunit alpha-1 | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | Amine oxidase [flavin-containing] A | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Estrogen receptor | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Sodium-dependent noradrenaline transporter | 2 |
| - | 10.6019/CHEMBL4651402 | SARS-CoV-2 | 2 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Histamine H2 receptor | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Adenosine receptor A1 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Cannabinoid receptor 1 | 2 |
Data from ChEMBL 36 via Core Engine