Assay Detail
Functional
CHEMBL2019173
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
20
Total Activities
20
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Tissue | Blood |
| 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 |
|---|---|---|---|
| Kd | 11 | 5.98 | 7.30 |
| pA2 | 9 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2018953 | — | — | 1 | 7.30 |
| CHEMBL2018954 | — | — | 1 | 6.60 |
| CHEMBL2018969 | — | — | 1 | 6.20 |
| CHEMBL2018968 | — | — | 1 | 6.20 |
| CHEMBL2018961 | — | — | 1 | 6.00 |
| CHEMBL2018964 | — | — | 1 | 6.00 |
| CHEMBL2018952 | — | — | 1 | 5.80 |
| CHEMBL2018967 | — | — | 1 | 5.70 |
| CHEMBL2018959 | — | — | 1 | 5.60 |
| CHEMBL2018955 | — | — | 1 | 5.20 |
| CHEMBL2018951 | — | — | 1 | 5.20 |
| CHEMBL2018957 | — | — | 1 | - |
| CHEMBL2018958 | — | — | 1 | - |
| CHEMBL2018960 | — | — | 1 | - |
| CHEMBL2016602 | — | — | 1 | - |
| CHEMBL2018962 | — | — | 1 | - |
| CHEMBL2018963 | — | — | 1 | - |
| CHEMBL2018965 | — | — | 1 | - |
| CHEMBL2018966 | — | — | 1 | - |
| CHEMBL2018956 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2018953 | — | Kd | = | 50.12 | nM | 7.30 |
| CHEMBL2018954 | — | Kd | = | 251.19 | nM | 6.60 |
| CHEMBL2018969 | — | Kd | = | 630.96 | nM | 6.20 |
| CHEMBL2018968 | — | Kd | = | 630.96 | nM | 6.20 |
| CHEMBL2018961 | — | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL2018964 | — | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL2018952 | — | Kd | = | 1584.89 | nM | 5.80 |
| CHEMBL2018967 | — | Kd | = | 1995.26 | nM | 5.70 |
| CHEMBL2018959 | — | Kd | = | 2511.89 | nM | 5.60 |
| CHEMBL2018955 | — | Kd | = | 6309.57 | nM | 5.20 |
| CHEMBL2018951 | — | Kd | = | 6309.57 | nM | 5.20 |
| CHEMBL2018957 | — | pA2 | - | — | - | |
| CHEMBL2018958 | — | pA2 | - | — | - | |
| CHEMBL2018960 | — | pA2 | - | — | - | |
| CHEMBL2016602 | — | pA2 | - | — | - | |
| CHEMBL2018962 | — | pA2 | - | — | - | |
| CHEMBL2018963 | — | pA2 | - | — | - | |
| CHEMBL2018965 | — | pA2 | - | — | - | |
| CHEMBL2018966 | — | pA2 | - | — | - | |
| CHEMBL2018956 | — | pA2 | - | — | - |