Compound Detail
CHEMBL855
TRIPROLIDINE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL855 |
| Name | TRIPROLIDINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | CBEQULMOCCWAQT-WOJGMQOQSA-N |
| Therapeutic | ✓ Yes |
3
Targets
7
Activities
3
Assay Types
5
PK Parameters
20
Publications
9
Known Names
1
Indications
Molecular Properties
278.4
MW (Da)
3.92
ALogP
2
HBA
0
HBD
16.1
PSA (Ų)
0.84
QED
0
Ro5 Violations
4
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1982 |
| Availability | Prescription |
| Chirality | Achiral |
Indications
Hypersensitivity
ATC Classification
R06AX07
triprolidine
Level 1: RESPIRATORY SYSTEM
Level 2: ANTIHISTAMINES FOR SYSTEMIC USE
Activity Summary
Kd 3 meas. best 9.9
IC50 2 meas.
Ki 2 meas. best 8.8
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Histamine H1 receptor CHEMBL3943 | Kd | 9.9 | 9.9 | 0.1 | 1 |
| Histamine H1 receptor CHEMBL231 | Ki | 8.8 | 8.8 | 1.6 | 1 |
| Histamine H1 receptor CHEMBL3943 | Ki | 8.78 | 8.78 | 1.7 | 1 |
| Unchecked CHEMBL612545 | Kd | 4.1 | 4.1 | 79000.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 8.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 8.0 | mL.min-1.g-1 | Homo sapiens |
| CL | 84.0 | uL.min-1.(10^6cells)-1 | Rattus norvegicus |
| T1/2 | 30.0 | hr | Homo sapiens |
| Vd | 8.7 | L.kg-1 | - |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Histamine H1 receptor | Kd | = | 0.1259 | nM | 9.9 | Potency against histamine H1 receptor on guinea pig ileum | 7650688 |
| Histamine H1 receptor | Ki | = | 1.6 | nM | 8.8 | Displacement of [3H]pyrilamine from histamine H1 receptor | 8496700 |
| Histamine H1 receptor | Ki | = | 1.66 | nM | 8.78 | Inhibition of [3H]mepyramine binding with histamine H1 receptor in guinea pig ce... | 7650688 |
| Unchecked | Kd | = | 79000.0 | nM | 4.1 | Stabilization of Red-dye-NHS fluorescent-labeled human LDH-Htr expressed in Esch... | 35074589 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| - | 10.6019/CHEMBL5724801 | Fibroblast | 304 |
| - | 10.6019/CHEMBL5058577 | HEK-293T | 304 |
| - | 10.6019/CHEMBL5058577 | U2OS | 304 |
| - | 10.6019/CHEMBL5058577 | Fibroblast | 304 |
| - | 10.6019/CHEMBL5724801 | HEK-293T | 304 |
| - | 10.6019/CHEMBL5724801 | U2OS | 304 |
| - | 10.5281/zenodo.13943903 | ADMET | 83 |
| 35074589 | 10.1016/j.ejmech.2022.114102 | Unchecked | 9 |
| - | 10.6019/CHEMBL5058564 | U2OS | 8 |
| - | 10.6019/CHEMBL5209801 | Glucagon-like peptide 1 receptor | 5 |
| - | 10.6019/CHEMBL5209801 | Glucose-dependent insulinotropic receptor | 5 |
| - | 10.6019/CHEMBL5209801 | Beta-2 adrenergic receptor | 5 |
| - | 10.6019/CHEMBL5058564 | Fibroblast | 5 |
| - | 10.6019/CHEMBL5209801 | Free fatty acid receptor 4 | 5 |
| - | 10.6019/CHEMBL5209801 | Adhesion G-protein coupled receptor F1 | 5 |
| - | 10.6019/CHEMBL5209801 | N-formyl peptide receptor 2 | 5 |
| - | 10.6019/CHEMBL5209801 | Alpha-2A adrenergic receptor | 5 |
| - | 10.6019/CHEMBL5209801 | Type-1 angiotensin II receptor | 5 |
| - | 10.6019/CHEMBL5209801 | CX3C chemokine receptor 1 | 5 |
| - | 10.6019/CHEMBL5209801 | Apelin receptor | 5 |
Data from ChEMBL 36 via Core Engine