Assay Detail
Functional
CHEMBL2019387
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Antagonist activity at CCR2 in human PBMC assessed as inhibition of MCP1-induced chemotaxis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of an orally-bioavailable CC Chemokine Receptor 2 antagonist derived from an acyclic diaminoalcohol backbone.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.75 | 8.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2018388 | — | — | 1 | 8.37 |
| CHEMBL2018385 | — | — | 1 | 8.30 |
| CHEMBL2018389 | — | — | 1 | 8.28 |
| CHEMBL2018394 | — | — | 1 | 8.14 |
| CHEMBL2018392 | — | — | 1 | 8.05 |
| CHEMBL2018387 | — | — | 1 | 8.00 |
| CHEMBL2018391 | — | — | 1 | 8.00 |
| CHEMBL2018402 | — | — | 1 | 7.92 |
| CHEMBL2018390 | — | — | 1 | 7.89 |
| CHEMBL2018400 | — | — | 1 | 7.85 |
| CHEMBL2018384 | — | — | 1 | 7.77 |
| CHEMBL2018396 | — | — | 1 | 7.70 |
| CHEMBL2018530 | — | — | 1 | 7.64 |
| CHEMBL2018401 | — | — | 1 | 7.64 |
| CHEMBL2018386 | — | — | 1 | 7.62 |
| CHEMBL2018380 | — | — | 1 | 7.50 |
| CHEMBL2018393 | — | — | 1 | 7.48 |
| CHEMBL2018395 | — | — | 1 | 7.13 |
| CHEMBL2018397 | — | — | 1 | 7.09 |
| CHEMBL2018370 | — | — | 1 | 6.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2018388 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL2018385 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2018389 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL2018394 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL2018392 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2018387 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL2018391 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2018402 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2018390 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2018400 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2018384 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL2018396 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2018530 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2018401 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2018386 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2018380 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL2018393 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL2018395 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL2018397 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL2018370 | — | IC50 | = | 240.0 | nM | 6.62 |