Assay Detail
Functional
CHEMBL3801465
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Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
10
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HuT78 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
2,8-Diazaspiro[4.5]decan-8-yl)pyrimidin-4-amine potent CCR4 antagonists capable of inducing receptor endocytosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 7.52 | 8.20 |
| Activity | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3799393 | — | — | 2 | 8.20 |
| CHEMBL2018953 | — | — | 1 | 8.00 |
| CHEMBL3798452 | — | — | 2 | 7.90 |
| CHEMBL3799578 | — | — | 2 | 7.80 |
| CHEMBL3797662 | — | — | 2 | 6.80 |
| CHEMBL3797462 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3799393 | — | EC50 | = | 6.31 | nM | 8.20 |
| CHEMBL2018953 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3798452 | — | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL3799578 | — | EC50 | = | 15.85 | nM | 7.80 |
| CHEMBL3797662 | — | EC50 | = | 158.49 | nM | 6.80 |
| CHEMBL3797462 | — | EC50 | = | 398.11 | nM | 6.40 |
| CHEMBL3798452 | — | Activity | = | 56.0 | % | - |
| CHEMBL3799393 | — | Activity | = | 64.0 | % | - |
| CHEMBL3799578 | — | Activity | = | 62.0 | % | - |
| CHEMBL3797662 | — | Activity | = | 74.0 | % | - |