Assay Detail
Binding
CHEMBL4630441
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Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CCRF-CEM |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel Piperidinyl-Azetidines as Potent and Selective CCR4 Antagonists Elicit Antitumor Response as a Single Agent and in Combination with Checkpoint Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.67 | 7.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4642563 | — | — | 1 | 7.44 |
| CHEMBL4641127 | — | — | 1 | 7.40 |
| CHEMBL4637143 | — | — | 1 | 7.30 |
| CHEMBL4645325 | — | — | 1 | 7.23 |
| CHEMBL4634054 | — | — | 1 | 7.13 |
| CHEMBL4639600 | — | — | 1 | 7.01 |
| CHEMBL4641873 | — | — | 1 | 6.96 |
| CHEMBL4636749 | — | — | 1 | 6.94 |
| CHEMBL4641595 | — | — | 1 | 6.88 |
| CHEMBL4647188 | — | — | 1 | 6.87 |
| CHEMBL4640439 | — | — | 1 | 6.61 |
| CHEMBL4647117 | — | — | 1 | 6.59 |
| CHEMBL4643158 | — | — | 1 | 6.43 |
| CHEMBL4637695 | — | — | 1 | 6.42 |
| CHEMBL4639418 | — | — | 1 | 6.39 |
| CHEMBL4633133 | — | — | 1 | 6.35 |
| CHEMBL4633494 | — | — | 1 | 6.28 |
| CHEMBL4638846 | — | — | 1 | 6.25 |
| CHEMBL4633920 | — | — | 1 | 6.24 |
| CHEMBL4643609 | — | — | 1 | 6.14 |
| CHEMBL4645037 | — | — | 1 | 6.11 |
| CHEMBL4640909 | — | — | 1 | 5.82 |
| CHEMBL4643839 | — | — | 1 | - |
| CHEMBL4644412 | — | — | 1 | - |
| CHEMBL4636965 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4642563 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4641127 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4637143 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4645325 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4634054 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4639600 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4641873 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL4636749 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL4641595 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL4647188 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL4640439 | — | IC50 | = | 247.0 | nM | 6.61 |
| CHEMBL4647117 | — | IC50 | = | 259.0 | nM | 6.59 |
| CHEMBL4643158 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4637695 | — | IC50 | = | 379.0 | nM | 6.42 |
| CHEMBL4639418 | — | IC50 | = | 409.0 | nM | 6.39 |
| CHEMBL4633133 | — | IC50 | = | 446.0 | nM | 6.35 |
| CHEMBL4633494 | — | IC50 | = | 523.0 | nM | 6.28 |
| CHEMBL4638846 | — | IC50 | = | 559.0 | nM | 6.25 |
| CHEMBL4633920 | — | IC50 | = | 575.0 | nM | 6.24 |
| CHEMBL4643609 | — | IC50 | = | 717.0 | nM | 6.14 |
| CHEMBL4645037 | — | IC50 | = | 775.0 | nM | 6.11 |
| CHEMBL4640909 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4643839 | — | IC50 | - | — | - | |
| CHEMBL4644412 | — | IC50 | - | — | - | |
| CHEMBL4636965 | — | IC50 | - | — | - |