Assay Detail
Functional
CHEMBL1174016
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at CCR5 expressed in CHO cells assessed as inhibition of RANTES-induced [35S]GTPgamma binding by scintillation proximity assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 1: Tuning the N-substituents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 8.14 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1172048 | — | — | 1 | 8.96 |
| CHEMBL1172043 | — | — | 1 | 8.96 |
| CHEMBL1172625 | — | — | 1 | 8.81 |
| CHEMBL1172050 | — | — | 1 | 8.79 |
| CHEMBL1172045 | — | — | 1 | 8.77 |
| CHEMBL1172051 | — | — | 1 | 8.77 |
| CHEMBL1172624 | — | — | 1 | 8.68 |
| CHEMBL1172046 | — | — | 1 | 8.57 |
| CHEMBL1172035 | NIFEVIROC | — | 1 | 8.54 |
| CHEMBL1172052 | — | — | 1 | 8.53 |
| CHEMBL1172047 | — | — | 1 | 8.49 |
| CHEMBL1172626 | — | — | 1 | 8.48 |
| CHEMBL1172157 | — | — | 1 | 8.46 |
| CHEMBL1171030 | — | — | 1 | 8.44 |
| CHEMBL1172623 | — | — | 1 | 8.40 |
| CHEMBL1172053 | — | — | 1 | 8.30 |
| CHEMBL1172439 | — | — | 1 | 8.28 |
| CHEMBL1172049 | — | — | 1 | 8.21 |
| CHEMBL1172036 | — | — | 1 | 8.21 |
| CHEMBL1172039 | — | — | 1 | 8.21 |
| CHEMBL1171965 | — | — | 1 | 8.06 |
| CHEMBL1171029 | — | — | 1 | 7.96 |
| CHEMBL1172438 | — | — | 1 | 7.84 |
| CHEMBL1169819 | — | — | 1 | 7.75 |
| CHEMBL1172044 | — | — | 1 | 7.70 |
| CHEMBL1172040 | — | — | 1 | 7.43 |
| CHEMBL1171966 | — | — | 1 | 7.42 |
| CHEMBL1172041 | — | — | 1 | 6.95 |
| CHEMBL1172037 | — | — | 1 | 6.91 |
| CHEMBL1172622 | — | — | 1 | 6.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1172048 | — | IC50 | = | 1.09 | nM | 8.96 |
| CHEMBL1172043 | — | IC50 | = | 1.09 | nM | 8.96 |
| CHEMBL1172625 | — | IC50 | = | 1.53 | nM | 8.81 |
| CHEMBL1172050 | — | IC50 | = | 1.62 | nM | 8.79 |
| CHEMBL1172045 | — | IC50 | = | 1.71 | nM | 8.77 |
| CHEMBL1172051 | — | IC50 | = | 1.69 | nM | 8.77 |
| CHEMBL1172624 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL1172046 | — | IC50 | = | 2.66 | nM | 8.57 |
| CHEMBL1172035 | NIFEVIROC | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL1172052 | — | IC50 | = | 2.93 | nM | 8.53 |
| CHEMBL1172047 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL1172626 | — | IC50 | = | 3.32 | nM | 8.48 |
| CHEMBL1172157 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL1171030 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL1172623 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1172053 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1172439 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL1172049 | — | IC50 | = | 6.15 | nM | 8.21 |
| CHEMBL1172036 | — | IC50 | = | 6.22 | nM | 8.21 |
| CHEMBL1172039 | — | IC50 | = | 6.15 | nM | 8.21 |
| CHEMBL1171965 | — | IC50 | = | 8.75 | nM | 8.06 |
| CHEMBL1171029 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1172438 | — | IC50 | = | 14.6 | nM | 7.84 |
| CHEMBL1169819 | — | IC50 | = | 17.8 | nM | 7.75 |
| CHEMBL1172044 | — | IC50 | = | 20.2 | nM | 7.70 |
| CHEMBL1172040 | — | IC50 | = | 37.3 | nM | 7.43 |
| CHEMBL1171966 | — | IC50 | = | 37.7 | nM | 7.42 |
| CHEMBL1172041 | — | IC50 | = | 113.6 | nM | 6.95 |
| CHEMBL1172037 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL1172622 | — | IC50 | = | 149.2 | nM | 6.83 |
| CHEMBL1172042 | — | IC50 | = | 220.6 | nM | 6.66 |
| CHEMBL1172038 | — | IC50 | > | 30.0 | nM | - |