Assay Detail
Binding
CHEMBL4380993
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition
12
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | LAD2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
C3a anaphylatoxin chemotactic receptor (CHEMBL4761) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Potent Thiophene Antagonists of Human Complement C3a Receptor with Anti-Inflammatory Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.87 | 8.70 |
| Inhibition | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4470864 | — | — | 3 | 8.70 |
| CHEMBL4576800 | — | — | 3 | 8.40 |
| CHEMBL4459627 | — | — | 3 | 8.10 |
| CHEMBL389348 | — | — | 3 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4470864 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4470864 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL4576800 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4576800 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL4459627 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4459627 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL389348 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL389348 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL389348 | — | Inhibition | - | % | - | |
| CHEMBL4576800 | — | Inhibition | - | % | - | |
| CHEMBL4459627 | — | Inhibition | - | % | - | |
| CHEMBL4470864 | — | Inhibition | - | % | - |