Assay Detail
Binding
CHEMBL649935
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Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Syntheses and SAR studies of 4-(heteroarylpiperdin-1-yl-methyl)-pyrrolidin-1-yl-acetic acid antagonists of the human CCR5 chemokine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 8.93 | 9.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL326487 | — | — | 1 | 9.64 |
| CHEMBL333619 | — | — | 1 | 9.64 |
| CHEMBL480503 | — | — | 1 | 9.54 |
| CHEMBL480693 | — | — | 1 | 9.47 |
| CHEMBL2112559 | — | — | 1 | 9.42 |
| CHEMBL513564 | — | — | 1 | 9.29 |
| CHEMBL2112558 | — | — | 1 | 9.24 |
| CHEMBL2112557 | — | — | 1 | 9.22 |
| CHEMBL520755 | — | — | 1 | 9.17 |
| CHEMBL2112552 | — | — | 1 | 9.15 |
| CHEMBL2112560 | — | — | 1 | 9.14 |
| CHEMBL2112553 | — | — | 1 | 9.12 |
| CHEMBL2112556 | — | — | 1 | 9.05 |
| CHEMBL2112555 | — | — | 1 | 9.00 |
| CHEMBL2112554 | — | — | 1 | 8.96 |
| CHEMBL481080 | — | — | 1 | 8.89 |
| CHEMBL481274 | — | — | 1 | 8.82 |
| CHEMBL480504 | — | — | 1 | 8.80 |
| CHEMBL511494 | — | — | 1 | 8.70 |
| CHEMBL471766 | — | — | 1 | 8.42 |
| CHEMBL511154 | — | — | 1 | 8.21 |
| CHEMBL471765 | — | — | 1 | 8.15 |
| CHEMBL471722 | — | — | 1 | 7.64 |
| CHEMBL470507 | — | — | 1 | 7.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL326487 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL333619 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL480503 | — | IC50 | = | 0.29 | nM | 9.54 |
| CHEMBL480693 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL2112559 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL513564 | — | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL2112558 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL2112557 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL520755 | — | IC50 | = | 0.67 | nM | 9.17 |
| CHEMBL2112552 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL2112560 | — | IC50 | = | 0.73 | nM | 9.14 |
| CHEMBL2112553 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL2112556 | — | IC50 | = | 0.89 | nM | 9.05 |
| CHEMBL2112555 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2112554 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL481080 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL481274 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL480504 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL511494 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL471766 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL511154 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL471765 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL471722 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL470507 | — | IC50 | = | 27.0 | nM | 7.57 |