Assay Detail
Functional
CHEMBL855766
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against human CCR8 expressed in CHO/Galpha16 cells assessed as inhibition of CCL1-induced increase of intracellular calcium by FLIPR assay
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO/Galpha16 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design, synthesis, and evaluation of naphthalene-sulfonamide antagonists of human CCR8.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 7.38 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL374939 | — | — | 1 | 9.52 |
| CHEMBL374527 | — | — | 1 | 8.38 |
| CHEMBL221790 | — | — | 1 | 8.29 |
| CHEMBL221586 | — | — | 1 | 8.21 |
| CHEMBL218297 | — | — | 1 | 8.16 |
| CHEMBL220652 | — | — | 1 | 8.12 |
| CHEMBL222062 | — | — | 1 | 8.02 |
| CHEMBL218369 | — | — | 1 | 8.01 |
| CHEMBL374978 | — | — | 1 | 7.97 |
| CHEMBL426551 | — | — | 1 | 7.90 |
| CHEMBL217984 | — | — | 1 | 7.84 |
| CHEMBL221601 | — | — | 1 | 7.82 |
| CHEMBL219380 | — | — | 1 | 7.72 |
| CHEMBL222020 | — | — | 1 | 7.71 |
| CHEMBL221639 | — | — | 1 | 7.70 |
| CHEMBL221842 | — | — | 1 | 7.69 |
| CHEMBL374414 | — | — | 1 | 7.63 |
| CHEMBL374274 | — | — | 1 | 7.61 |
| CHEMBL221712 | — | — | 1 | 7.54 |
| CHEMBL219431 | — | — | 1 | 7.44 |
| CHEMBL221650 | — | — | 1 | 7.43 |
| CHEMBL218298 | — | — | 1 | 7.38 |
| CHEMBL374964 | — | — | 1 | 7.36 |
| CHEMBL217909 | — | — | 1 | 7.33 |
| CHEMBL218554 | — | — | 1 | 7.24 |
| CHEMBL221978 | — | — | 1 | 7.22 |
| CHEMBL217965 | — | — | 1 | 7.00 |
| CHEMBL220650 | — | — | 1 | 6.84 |
| CHEMBL412116 | — | — | 1 | 6.82 |
| CHEMBL218209 | — | — | 1 | 6.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL374939 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL374527 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL221790 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL221586 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL218297 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL220652 | — | IC50 | = | 7.65 | nM | 8.12 |
| CHEMBL222062 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL218369 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL374978 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL426551 | — | IC50 | = | 12.5 | nM | 7.90 |
| CHEMBL217984 | — | IC50 | = | 14.5 | nM | 7.84 |
| CHEMBL221601 | — | IC50 | = | 15.3 | nM | 7.82 |
| CHEMBL219380 | — | IC50 | = | 19.2 | nM | 7.72 |
| CHEMBL222020 | — | IC50 | = | 19.6 | nM | 7.71 |
| CHEMBL221639 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL221842 | — | IC50 | = | 20.4 | nM | 7.69 |
| CHEMBL374414 | — | IC50 | = | 23.6 | nM | 7.63 |
| CHEMBL374274 | — | IC50 | = | 24.6 | nM | 7.61 |
| CHEMBL221712 | — | IC50 | = | 28.6 | nM | 7.54 |
| CHEMBL219431 | — | IC50 | = | 36.1 | nM | 7.44 |
| CHEMBL221650 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL218298 | — | IC50 | = | 41.7 | nM | 7.38 |
| CHEMBL374964 | — | IC50 | = | 43.9 | nM | 7.36 |
| CHEMBL217909 | — | IC50 | = | 46.9 | nM | 7.33 |
| CHEMBL218554 | — | IC50 | = | 57.9 | nM | 7.24 |
| CHEMBL221978 | — | IC50 | = | 59.5 | nM | 7.22 |
| CHEMBL217965 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL220650 | — | IC50 | = | 144.5 | nM | 6.84 |
| CHEMBL412116 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL218209 | — | IC50 | = | 205.9 | nM | 6.69 |
| CHEMBL441870 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL376517 | — | IC50 | = | 365.0 | nM | 6.44 |
| CHEMBL376071 | — | IC50 | = | 367.7 | nM | 6.43 |
| CHEMBL220651 | — | IC50 | = | 612.5 | nM | 6.21 |
| CHEMBL385654 | — | IC50 | = | 638.5 | nM | 6.20 |
| CHEMBL218555 | — | IC50 | = | 885.1 | nM | 6.05 |
| CHEMBL222112 | — | IC50 | = | 1004.0 | nM | 6.00 |
| CHEMBL219432 | — | IC50 | = | 1519.0 | nM | 5.82 |
| CHEMBL376070 | — | IC50 | > | 1900.0 | nM | - |
| CHEMBL374963 | — | IC50 | > | 3300.0 | nM | - |
| CHEMBL221841 | — | IC50 | > | 3300.0 | nM | - |