Assay Detail
Functional
CHEMBL3387988
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay
22
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
C3a anaphylatoxin chemotactic receptor (CHEMBL4761) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Potent heterocyclic ligands for human complement c3a receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.07 | 9.10 |
| pIC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3342676 | — | — | 2 | 9.10 |
| CHEMBL3342678 | — | — | 2 | 8.40 |
| CHEMBL3342677 | — | — | 2 | 8.22 |
| CHEMBL3342680 | — | — | 2 | 6.00 |
| CHEMBL3342681 | — | — | 2 | 6.00 |
| CHEMBL389348 | — | — | 2 | 5.90 |
| CHEMBL230034 | — | — | 2 | 5.75 |
| CHEMBL3342683 | — | — | 2 | 5.70 |
| CHEMBL3342679 | — | — | 2 | 5.54 |
| CHEMBL3342682 | — | — | 2 | 4.72 |
| CHEMBL3342684 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3342676 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3342678 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3342677 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3342676 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL3342681 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3342680 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3342681 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL389348 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL3342680 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL230034 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3342683 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL3342683 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL230034 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL3342679 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL3342678 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL3342679 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL3342677 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL3342682 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL3342682 | — | IC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL389348 | — | IC50 | = | 1.3 | nM | - |
| CHEMBL3342684 | — | pIC50 | - | — | - | |
| CHEMBL3342684 | — | IC50 | - | — | - |