Compound Detail
CHEMBL811
BROMPHENIRAMINE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL811 |
| Name | BROMPHENIRAMINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | ZDIGNSYAACHWNL-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
5
Targets
6
Activities
1
Assay Types
3
PK Parameters
20
Publications
8
Known Names
1
Indications
Molecular Properties
319.2
MW (Da)
3.93
ALogP
2
HBA
0
HBD
16.1
PSA (Ų)
0.83
QED
0
Ro5 Violations
5
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1957 |
| Availability | Prescription |
| Chirality | Racemic |
Indications
Hypersensitivity
ATC Classification
R06AB01
brompheniramine
Level 1: RESPIRATORY SYSTEM
Level 2: ANTIHISTAMINES FOR SYSTEMIC USE
R06AB51
brompheniramine, combinations
Level 1: RESPIRATORY SYSTEM
Level 2: ANTIHISTAMINES FOR SYSTEMIC USE
Activity Summary
IC50 6 meas. best 6.52
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Sodium-dependent serotonin transporter CHEMBL313 | IC50 | 6.52 | 6.52 | 300.0 | 1 |
| Voltage-gated inwardly rectifying potassium channel KCNH2 CHEMBL240 | IC50 | 6.05 | 6.05 | 891.2 | 1 |
| Norepinephrine transporter CHEMBL304 | IC50 | 5.33 | 5.33 | 4700.0 | 1 |
| Sodium channel alpha subunits; brain (Types I, II, III) CHEMBL2096682 | IC50 | 4.96 | 4.88 | 11000.0 | 2 |
| Voltage-dependent L-type calcium channel subunit alpha-1C CHEMBL3762 | IC50 | 4.79 | 4.79 | 16120.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| Cmax | 36.0 | nM | Homo sapiens |
| T1/2 | 24.9 | hr | Homo sapiens |
| Vd | 10.0 | L.kg-1 | - |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Sodium-dependent serotonin transporter | IC50 | = | 300.0 | nM | 6.52 | In vitro inhibition of accumulation of [14C]5-HT (5-HT) in mouse brain slices | 6458703 |
| Voltage-gated inwardly rectifying potassium channel KCNH2 | IC50 | = | 891.25 | nM | 6.05 | Inhibition of human ERG | 21185626 |
| Norepinephrine transporter | IC50 | = | 4700.0 | nM | 5.33 | In vitro inhibition of accumulation of (-)-[3H]Norepinephrine (NA) in mouse brai... | 6458703 |
| Sodium channel alpha subunits; brain (Types I, II, III) | IC50 | = | 11000.0 | nM | 4.96 | Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on vol... | 2579237 |
| Sodium channel alpha subunits; brain (Types I, II, III) | IC50 | = | 16000.0 | nM | 4.8 | Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on vol... | 2579237 |
| Voltage-dependent L-type calcium channel subunit alpha-1C | IC50 | = | 16120.0 | nM | 4.79 | Inhibition of Cav1.2 calcium current measured using whole cell patch clamp in ra... | - |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 2579237 | 10.1021/jm00381a019 | Sodium channel alpha subunits; brain (Types I, II, III) | 4 |
| 37468498 | 10.1038/s41467-023-40064-9 | Alpha-1A adrenergic receptor | 4 |
| 37468498 | 10.1038/s41467-023-40064-9 | Muscarinic acetylcholine receptor M2 | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | Progesterone receptor | 3 |
| 2570152 | 10.1021/jm00129a026 | Cavia porcellus | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | Androgen receptor | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 2B | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 1A | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | Muscarinic acetylcholine receptor M1 | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | Alpha-2A adrenergic receptor | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | Nuclear receptor subfamily 1 group I member 2 | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | Prostaglandin G/H synthase 1 | 3 |
| 6458703 | 10.1021/jm00144a025 | Sodium-dependent serotonin transporter | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Peroxisome proliferator-activated receptor gamma | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Adenosine receptor A3 | 2 |
| 26948801 | 10.1016/j.drudis.2016.02.015 | Homo sapiens | 2 |
| 24799086 | 10.1002/hep.27206 | Homo sapiens | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Mu-type opioid receptor | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Sodium-dependent noradrenaline transporter | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Sodium-dependent serotonin transporter | 2 |
Data from ChEMBL 36 via Core Engine