Compound Detail
CHEMBL278398
PHENINDAMINE 🧪 Phase II
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🧪 Phase II
Basic Information
| ChEMBL ID | CHEMBL278398 |
| Name | PHENINDAMINE |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | ISFHAYSTHMVOJR-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
1
Targets
3
Activities
3
Assay Types
0
PK Parameters
20
Publications
3
Known Names
1
Indications
1
Mechanisms
Molecular Properties
261.4
MW (Da)
3.92
ALogP
1
HBA
0
HBD
3.2
PSA (Ų)
0.75
QED
0
Ro5 Violations
1
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Racemic |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Histamine H1 receptor antagonist | ANTAGONIST | Histamine H1 receptor | ✓ | ✓ |
Indications
Hypersensitivity
ATC Classification
R06AX04
phenindamine
Level 1: RESPIRATORY SYSTEM
Level 2: ANTIHISTAMINES FOR SYSTEMIC USE
Activity Summary
IC50 1 meas. best 7.44
Kd 1 meas. best 8.8
Ki 1 meas. best 8.2
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Histamine H1 receptor CHEMBL3943 | Kd | 8.8 | 8.8 | 1.6 | 1 |
| Histamine H1 receptor CHEMBL3943 | Ki | 8.2 | 8.2 | 6.3 | 1 |
| Histamine H1 receptor CHEMBL3943 | IC50 | 7.44 | 7.44 | 36.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Histamine H1 receptor | Kd | = | 1.585 | nM | 8.8 | Potency against histamine H1 receptor on guinea pig ileum | 7650688 |
| Histamine H1 receptor | Ki | = | 6.31 | nM | 8.2 | Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig ce... | 7650688 |
| Histamine H1 receptor | IC50 | = | 36.0 | nM | 7.44 | In vitro antagonistic activity at the Histamine H1 receptor in guinea pig ileum | 10866399 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 37468498 | 10.1038/s41467-023-40064-9 | Muscarinic acetylcholine receptor M2 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 1A | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 2A | 2 |
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 2 |
| - | 10.6019/CHEMBL4651402 | SARS-CoV-2 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Alpha-2A adrenergic receptor | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Progesterone receptor | 2 |
| 7650688 | 10.1021/jm00017a019 | Histamine H1 receptor | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 2B | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Gamma-aminobutyric acid receptor subunit alpha-1 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Beta-1 adrenergic receptor | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Adenosine receptor A3 | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Adenosine receptor A1 | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Neuronal acetylcholine receptor subunit alpha-4 | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Sodium-dependent dopamine transporter | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Beta-2 adrenergic receptor | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Voltage-dependent L-type calcium channel subunit alpha-1C | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Voltage-gated inwardly rectifying potassium channel KCNH2 | 1 |
| - | 10.21203/rs.3.rs-23951/v1 | SARS-CoV-2 | 1 |
| 20020916 | 10.1080/15376510701857262 | Phospholipidosis | 1 |
Data from ChEMBL 36 via Core Engine