Assay Detail
Binding
CHEMBL3367645
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Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
19
Total Activities
19
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Lead identification of benzimidazolone and azabenzimidazolone arylsulfonamides as CC-chemokine receptor 4 (CCR4) antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 10 | 6.02 | 7.30 |
| pA2 | 9 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2018953 | — | — | 1 | 7.30 |
| CHEMBL2018954 | — | — | 1 | 6.60 |
| CHEMBL3310839 | — | — | 1 | 6.10 |
| CHEMBL3310840 | — | — | 1 | 5.60 |
| CHEMBL3310826 | — | — | 1 | 5.30 |
| CHEMBL3310841 | — | — | 1 | 5.20 |
| CHEMBL3310825 | — | — | 1 | - |
| CHEMBL3310827 | — | — | 1 | - |
| CHEMBL3310828 | — | — | 1 | - |
| CHEMBL3310838 | — | — | 1 | - |
| CHEMBL3310837 | — | — | 1 | - |
| CHEMBL3310836 | — | — | 1 | - |
| CHEMBL3310835 | — | — | 1 | - |
| CHEMBL3310834 | — | — | 1 | - |
| CHEMBL3310833 | — | — | 1 | - |
| CHEMBL3310832 | — | — | 1 | - |
| CHEMBL3310831 | — | — | 1 | - |
| CHEMBL3310830 | — | — | 1 | - |
| CHEMBL3310829 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2018953 | — | Kd | = | 50.12 | nM | 7.30 |
| CHEMBL2018954 | — | Kd | = | 251.19 | nM | 6.60 |
| CHEMBL3310839 | — | Kd | = | 794.33 | nM | 6.10 |
| CHEMBL3310840 | — | Kd | = | 2511.89 | nM | 5.60 |
| CHEMBL3310826 | — | Kd | = | 5011.87 | nM | 5.30 |
| CHEMBL3310841 | — | Kd | = | 6309.57 | nM | 5.20 |
| CHEMBL3310825 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL3310827 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL3310828 | — | pA2 | - | — | - | |
| CHEMBL3310838 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL3310837 | — | pA2 | - | — | - | |
| CHEMBL3310836 | — | pA2 | - | — | - | |
| CHEMBL3310835 | — | pA2 | - | — | - | |
| CHEMBL3310834 | — | pA2 | - | — | - | |
| CHEMBL3310833 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL3310832 | — | pA2 | - | — | - | |
| CHEMBL3310831 | — | pA2 | - | — | - | |
| CHEMBL3310830 | — | pA2 | - | — | - | |
| CHEMBL3310829 | — | pA2 | - | — | - |