Assay Detail
Functional
CHEMBL933958
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human CCR2 in THP1 cells assessed as inhibition of MCP1-induced chemotaxis
63
Total Activities
63
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | THP-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Potent antagonists of the CCR2b receptor. Part 3: SAR of the (R)-3-aminopyrrolidine series.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 63 | 7.49 | 9.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL256629 | — | — | 1 | 9.08 |
| CHEMBL271288 | — | — | 1 | 9.05 |
| CHEMBL271289 | — | — | 1 | 8.59 |
| CHEMBL271290 | — | — | 1 | 8.51 |
| CHEMBL404259 | — | — | 1 | 8.44 |
| CHEMBL257066 | — | — | 1 | 8.41 |
| CHEMBL257064 | — | — | 1 | 8.29 |
| CHEMBL402723 | — | — | 1 | 8.26 |
| CHEMBL403281 | — | — | 1 | 8.21 |
| CHEMBL270435 | — | — | 1 | 8.06 |
| CHEMBL404269 | — | — | 1 | 8.04 |
| CHEMBL405633 | — | — | 1 | 8.03 |
| CHEMBL257062 | — | — | 1 | 7.96 |
| CHEMBL257063 | — | — | 1 | 7.96 |
| CHEMBL271725 | — | — | 1 | 7.92 |
| CHEMBL257065 | — | — | 1 | 7.91 |
| CHEMBL255209 | — | — | 1 | 7.85 |
| CHEMBL337246 | — | — | 1 | 7.80 |
| CHEMBL408908 | — | — | 1 | 7.75 |
| CHEMBL257316 | — | — | 1 | 7.68 |
| CHEMBL270005 | — | — | 1 | 7.68 |
| CHEMBL272284 | — | — | 1 | 7.66 |
| CHEMBL255408 | — | — | 1 | 7.62 |
| CHEMBL271935 | — | — | 1 | 7.46 |
| CHEMBL272283 | — | — | 1 | 7.37 |
| CHEMBL404837 | — | — | 1 | 7.37 |
| CHEMBL439062 | — | — | 1 | 7.13 |
| CHEMBL272331 | — | — | 1 | 7.11 |
| CHEMBL270182 | — | — | 1 | 6.99 |
| CHEMBL257702 | — | — | 1 | 6.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL256629 | — | IC50 | = | 0.83 | nM | 9.08 |
| CHEMBL271288 | — | IC50 | = | 0.89 | nM | 9.05 |
| CHEMBL271289 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL271290 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL404259 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL257066 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL257064 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL402723 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL403281 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL270435 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL404269 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL405633 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL257063 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL257062 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL271725 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL257065 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL255209 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL337246 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL408908 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL257316 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL270005 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL272284 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL255408 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL271935 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL404837 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL272283 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL439062 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL272331 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL270182 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL257702 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL272543 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL402322 | — | IC50 | = | 286.0 | nM | 6.54 |
| CHEMBL273195 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL439252 | — | IC50 | = | 418.0 | nM | 6.38 |
| CHEMBL410829 | — | IC50 | = | 418.0 | nM | 6.38 |
| CHEMBL257510 | — | IC50 | = | 445.0 | nM | 6.35 |
| CHEMBL258364 | — | IC50 | = | 473.0 | nM | 6.33 |
| CHEMBL403424 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL256256 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL271726 | — | IC50 | - | — | - | |
| CHEMBL257866 | — | IC50 | - | — | - | |
| CHEMBL402988 | — | IC50 | - | — | - | |
| CHEMBL429912 | — | IC50 | - | — | - | |
| CHEMBL255585 | — | IC50 | - | — | - | |
| CHEMBL257511 | — | IC50 | - | — | - | |
| CHEMBL255385 | — | IC50 | - | — | - | |
| CHEMBL272495 | — | IC50 | - | — | - | |
| CHEMBL272496 | — | IC50 | - | — | - | |
| CHEMBL271494 | — | IC50 | - | — | - | |
| CHEMBL409679 | — | IC50 | - | — | - |