Compound Detail
CHEMBL1241
TRIPELENNAMINE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL1241 |
| Name | TRIPELENNAMINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | UFLGIAIHIAPJJC-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
20
Publications
3
Known Names
2
Indications
Molecular Properties
255.4
MW (Da)
2.65
ALogP
3
HBA
0
HBD
19.4
PSA (Ų)
0.79
QED
0
Ro5 Violations
6
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1948 |
| Availability | Discontinued |
| Chirality | Achiral |
Indications
Hypersensitivity Pruritus
ATC Classification
D04AA04
tripelennamine
Level 1: DERMATOLOGICALS
Level 2: ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC.
R06AC04
tripelennamine
Level 1: RESPIRATORY SYSTEM
Level 2: ANTIHISTAMINES FOR SYSTEMIC USE
Activity Summary
IC50 1 meas. best 7.4
Ki 1 meas.
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Histamine H1 receptor CHEMBL231 | IC50 | 7.4 | 7.4 | 39.8 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Histamine H1 receptor | IC50 | = | 39.81 | nM | 7.4 | Inhibitory activity against human Histamine H1 receptor | 14667234 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 15646539 | 10.1016/s0399-8320(04)95062-2 | Unchecked | 11 |
| 15646539 | 10.1016/s0399-8320(04)95062-2 | NON-PROTEIN TARGET | 8 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 1A | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 2B | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | Gamma-aminobutyric acid receptor subunit alpha-1 | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | Progesterone receptor | 3 |
| 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-2A adrenergic receptor | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | Alpha-1A adrenergic receptor | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | Muscarinic acetylcholine receptor M2 | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | Thromboxane A2 receptor | 3 |
| 14667234 | 10.1021/jm030936t | Histamine H1 receptor | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | Sodium-dependent serotonin transporter | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Mu-type opioid receptor | 2 |
| 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 |
| 38318365 | 10.1016/j.isci.2024.108907 | Deoxynucleoside triphosphate triphosphohydrolase SAMHD1 | 2 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
Data from ChEMBL 36 via Core Engine