Assay Detail
Binding
CHEMBL933957
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Displacement of [125I]MCP1 from human CCR2b in THP1 cells
61
Total Activities
61
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 61 | 6.71 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL256629 | — | — | 1 | 8.49 |
| CHEMBL257062 | — | — | 1 | 8.39 |
| CHEMBL270435 | — | — | 1 | 8.28 |
| CHEMBL271725 | — | — | 1 | 8.21 |
| CHEMBL271288 | — | — | 1 | 7.96 |
| CHEMBL408908 | — | — | 1 | 7.85 |
| CHEMBL257066 | — | — | 1 | 7.72 |
| CHEMBL257063 | — | — | 1 | 7.70 |
| CHEMBL271290 | — | — | 1 | 7.70 |
| CHEMBL404259 | — | — | 1 | 7.58 |
| CHEMBL255209 | — | — | 1 | 7.41 |
| CHEMBL257064 | — | — | 1 | 7.38 |
| CHEMBL404269 | — | — | 1 | 7.28 |
| CHEMBL337246 | — | — | 1 | 7.27 |
| CHEMBL405633 | — | — | 1 | 7.23 |
| CHEMBL272283 | — | — | 1 | 7.06 |
| CHEMBL270205 | — | — | 1 | 7.02 |
| CHEMBL271289 | — | — | 1 | 6.94 |
| CHEMBL257065 | — | — | 1 | 6.94 |
| CHEMBL271935 | — | — | 1 | 6.94 |
| CHEMBL403281 | — | — | 1 | 6.92 |
| CHEMBL272331 | — | — | 1 | 6.82 |
| CHEMBL257316 | — | — | 1 | 6.78 |
| CHEMBL255408 | — | — | 1 | 6.75 |
| CHEMBL270005 | — | — | 1 | 6.69 |
| CHEMBL404837 | — | — | 1 | 6.68 |
| CHEMBL402723 | — | — | 1 | 6.65 |
| CHEMBL255585 | — | — | 1 | 6.52 |
| CHEMBL402322 | — | — | 1 | 6.52 |
| CHEMBL272284 | — | — | 1 | 6.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL256629 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL257062 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL270435 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL271725 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL271288 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL408908 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL257066 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL257063 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL271290 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL404259 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL255209 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL257064 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL404269 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL337246 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL405633 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL272283 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL270205 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL271289 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL257065 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL271935 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL403281 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL272331 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL257316 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL255408 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL270005 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL404837 | — | IC50 | = | 208.0 | nM | 6.68 |
| CHEMBL402723 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL255585 | — | IC50 | = | 305.0 | nM | 6.52 |
| CHEMBL402322 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL272284 | — | IC50 | = | 308.0 | nM | 6.51 |
| CHEMBL273195 | — | IC50 | = | 489.0 | nM | 6.31 |
| CHEMBL270182 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL439252 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL404260 | — | IC50 | = | 643.0 | nM | 6.19 |
| CHEMBL410829 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL272330 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL439062 | — | IC50 | = | 759.0 | nM | 6.12 |
| CHEMBL258364 | — | IC50 | = | 785.0 | nM | 6.11 |
| CHEMBL257510 | — | IC50 | = | 832.0 | nM | 6.08 |
| CHEMBL272543 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL257702 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL272542 | — | IC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL257511 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL405632 | — | IC50 | = | 2380.0 | nM | 5.62 |
| CHEMBL271726 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL255385 | — | IC50 | = | 2650.0 | nM | 5.58 |
| CHEMBL402988 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL429912 | — | IC50 | = | 3170.0 | nM | 5.50 |
| CHEMBL403058 | — | IC50 | = | 4330.0 | nM | 5.36 |
| CHEMBL442451 | — | IC50 | = | 10000.0 | nM | 5.00 |