Assay Detail
Functional
CHEMBL4630442
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
31
Total Activities
31
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
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 | 31 | 7.23 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4641127 | — | — | 1 | 8.22 |
| CHEMBL4642563 | — | — | 1 | 8.10 |
| CHEMBL4637695 | — | — | 1 | 8.05 |
| CHEMBL4645325 | — | — | 1 | 7.75 |
| CHEMBL4639600 | — | — | 1 | 7.68 |
| CHEMBL4637143 | — | — | 1 | 7.66 |
| CHEMBL4647117 | — | — | 1 | 7.66 |
| CHEMBL4641595 | — | — | 1 | 7.64 |
| CHEMBL4634054 | — | — | 1 | 7.62 |
| CHEMBL4633133 | — | — | 1 | 7.60 |
| CHEMBL4633494 | — | — | 1 | 7.55 |
| CHEMBL4647188 | — | — | 1 | 7.54 |
| CHEMBL4636749 | — | — | 1 | 7.51 |
| CHEMBL4645037 | — | — | 1 | 7.44 |
| CHEMBL4641873 | — | — | 1 | 7.43 |
| CHEMBL4640439 | — | — | 1 | 7.38 |
| CHEMBL4639418 | — | — | 1 | 7.33 |
| CHEMBL4638846 | — | — | 1 | 7.16 |
| CHEMBL4633920 | — | — | 1 | 7.11 |
| CHEMBL4643609 | — | — | 1 | 7.08 |
| CHEMBL4643158 | — | — | 1 | 7.04 |
| CHEMBL4649666 | — | — | 1 | 6.92 |
| CHEMBL4640909 | — | — | 1 | 6.43 |
| CHEMBL4642090 | — | — | 1 | 6.34 |
| CHEMBL4644412 | — | — | 1 | 6.30 |
| CHEMBL4643066 | — | — | 1 | 6.22 |
| CHEMBL4635359 | — | — | 1 | 5.86 |
| CHEMBL4643839 | — | — | 1 | 5.83 |
| CHEMBL4636965 | — | — | 1 | - |
| CHEMBL4645456 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4641127 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4642563 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4637695 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4645325 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4639600 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4637143 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4647117 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4641595 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4634054 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4633133 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4633494 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4647188 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4636749 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4645037 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4641873 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4640439 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4639418 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4638846 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4633920 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4643609 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4643158 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL4649666 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL4640909 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4642090 | — | IC50 | = | 455.0 | nM | 6.34 |
| CHEMBL4644412 | — | IC50 | = | 505.0 | nM | 6.30 |
| CHEMBL4643066 | — | IC50 | = | 596.0 | nM | 6.22 |
| CHEMBL4635359 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL4643839 | — | IC50 | = | 1470.0 | nM | 5.83 |
| CHEMBL4636965 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4645456 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4641721 | — | IC50 | > | 5000.0 | nM | - |