Compound Detail
CHEMBL2107783
TAPRENEPAG 🧪 Phase II
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🧪 Phase II
Basic Information
| ChEMBL ID | CHEMBL2107783 |
| Name | TAPRENEPAG |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | MFFBXYNKZHTCEY-UHFFFAOYSA-N |
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
20
Publications
4
Known Names
Molecular Properties
478.5
MW (Da)
3.12
ALogP
7
HBA
1
HBD
114.6
PSA (Ų)
0.37
QED
0
Ro5 Violations
10
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Achiral |
Activity Summary
EC50 1 meas. best 8.55
Ki 1 meas. best 8.0
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Prostaglandin E2 receptor EP2 subtype CHEMBL1881 | EC50 | 8.55 | 8.55 | 2.8 | 1 |
| Prostaglandin E2 receptor EP2 subtype CHEMBL1881 | Ki | 8.0 | 8.0 | 10.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Prostaglandin E2 receptor EP2 subtype | EC50 | = | 2.8 | nM | 8.55 | Agonist activity at EP2 receptor (unknown origin) by functional assay | 24279689 |
| Prostaglandin E2 receptor EP2 subtype | Ki | = | 10.0 | nM | 8.0 | Binding affinity to EP2 receptor (unknown origin) by competitive binding assay | 24279689 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| - | 10.6019/CHEMBL5724696 | U2OS | 24 |
| - | 10.6019/CHEMBL4689842 | HEK-293T | 10 |
| - | 10.6019/CHEMBL4689842 | U2OS | 9 |
| - | 10.6019/CHEMBL4689842 | Fibroblast | 9 |
| - | 10.6019/CHEMBL5209801 | Beta-2 adrenergic receptor | 5 |
| - | 10.6019/CHEMBL5209801 | N-formyl peptide receptor 2 | 5 |
| - | 10.6019/CHEMBL5209801 | Glucose-dependent insulinotropic receptor | 5 |
| - | 10.6019/CHEMBL5209801 | Alpha-2A adrenergic receptor | 5 |
| - | 10.6019/CHEMBL5209801 | Free fatty acid receptor 4 | 5 |
| - | 10.6019/CHEMBL5209801 | Apelin receptor | 5 |
| - | 10.6019/CHEMBL5209801 | C5a anaphylatoxin chemotactic receptor 1 | 5 |
| - | 10.6019/CHEMBL5209801 | CX3C chemokine receptor 1 | 5 |
| - | 10.6019/CHEMBL5209801 | Sphingosine 1-phosphate receptor 1 | 5 |
| - | 10.6019/CHEMBL5209801 | Glucagon-like peptide 1 receptor | 5 |
| - | 10.6019/CHEMBL5209801 | Type-1 angiotensin II receptor | 5 |
| - | 10.6019/CHEMBL5209801 | Adhesion G-protein coupled receptor F1 | 5 |
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 4 |
| 24279689 | 10.1021/jm401431x | Unchecked | 3 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
| 24279689 | 10.1021/jm401431x | Prostacyclin receptor | 2 |
Data from ChEMBL 36 via Core Engine