Assay Detail
Binding
CHEMBL654654
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Displacement inhibition of 125-I labeled MIP-alpha from CCR5 receptor expressed on CHO cell membranes
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
1,3,4 Trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 8.38 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL344261 | — | — | 1 | 9.40 |
| CHEMBL344641 | — | — | 1 | 9.30 |
| CHEMBL328297 | — | — | 1 | 9.10 |
| CHEMBL275998 | — | — | 1 | 9.10 |
| CHEMBL137327 | — | — | 1 | 8.96 |
| CHEMBL342842 | — | — | 1 | 8.92 |
| CHEMBL343745 | — | — | 1 | 8.92 |
| CHEMBL343366 | — | — | 1 | 8.82 |
| CHEMBL138437 | — | — | 1 | 8.80 |
| CHEMBL335562 | — | — | 1 | 8.77 |
| CHEMBL428104 | — | — | 1 | 8.74 |
| CHEMBL343160 | — | — | 1 | 8.41 |
| CHEMBL137728 | — | — | 1 | 8.30 |
| CHEMBL137419 | — | — | 1 | 8.22 |
| CHEMBL137038 | — | — | 1 | 8.18 |
| CHEMBL137524 | — | — | 1 | 8.05 |
| CHEMBL136977 | — | — | 1 | 8.05 |
| CHEMBL138645 | — | — | 1 | 8.00 |
| CHEMBL135432 | — | — | 1 | 7.92 |
| CHEMBL137072 | — | — | 1 | 7.92 |
| CHEMBL138282 | — | — | 1 | 7.85 |
| CHEMBL137272 | — | — | 1 | 7.68 |
| CHEMBL137206 | — | — | 1 | 7.64 |
| CHEMBL137154 | — | — | 1 | 7.38 |
| CHEMBL137650 | — | — | 1 | 7.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL344261 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL344641 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL328297 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL275998 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL137327 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL342842 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL343745 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL343366 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL138437 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL335562 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL428104 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL343160 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL137728 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL137419 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL137038 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL137524 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL136977 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL138645 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL135432 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL137072 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL138282 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL137272 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL137206 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL137154 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL137650 | — | IC50 | = | 66.0 | nM | 7.18 |