Assay Detail
Binding
CHEMBL2019171
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Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
20
Total Activities
20
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Lead optimisation of the N1 substituent of a novel series of indazole arylsulfonamides as CCR4 antagonists and identification of a candidate for clinical investigation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.31 | 9.10 |
| pKi | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2018953 | — | — | 1 | 9.10 |
| CHEMBL2018954 | — | — | 1 | 8.50 |
| CHEMBL2018968 | — | — | 1 | 8.10 |
| CHEMBL2018969 | — | — | 1 | 8.00 |
| CHEMBL2018964 | — | — | 1 | 7.90 |
| CHEMBL2018967 | — | — | 1 | 7.80 |
| CHEMBL2018959 | — | — | 1 | 7.70 |
| CHEMBL2018951 | — | — | 1 | 7.40 |
| CHEMBL2018952 | — | — | 1 | 7.40 |
| CHEMBL2016602 | — | — | 1 | 7.30 |
| CHEMBL2018961 | — | — | 1 | 7.00 |
| CHEMBL2018957 | — | — | 1 | 6.90 |
| CHEMBL2018966 | — | — | 1 | 6.80 |
| CHEMBL2018956 | — | — | 1 | 6.80 |
| CHEMBL2018958 | — | — | 1 | 6.60 |
| CHEMBL2018960 | — | — | 1 | 6.60 |
| CHEMBL2018955 | — | — | 1 | 6.60 |
| CHEMBL2018962 | — | — | 1 | 6.50 |
| CHEMBL2018963 | — | — | 1 | 5.90 |
| CHEMBL2018965 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2018953 | — | Ki | = | 0.7943 | nM | 9.10 |
| CHEMBL2018954 | — | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL2018968 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL2018969 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2018964 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL2018967 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL2018959 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL2018951 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL2018952 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL2016602 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL2018961 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL2018957 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL2018966 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL2018956 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL2018958 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL2018960 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL2018955 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL2018962 | — | Ki | = | 316.23 | nM | 6.50 |
| CHEMBL2018963 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL2018965 | — | pKi | - | — | - |