Assay Detail
Binding
CHEMBL649953
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Ability to inhibit [125I]-labeled RANTES binding to the CCR5 receptor expressed in membrane preparations from CHO cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 8.11 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL140827 | — | — | 1 | 9.15 |
| CHEMBL113436 | — | — | 1 | 8.70 |
| CHEMBL334470 | — | — | 1 | 8.57 |
| CHEMBL138502 | — | — | 1 | 8.28 |
| CHEMBL322251 | — | — | 1 | 8.15 |
| CHEMBL342137 | — | — | 1 | 8.00 |
| CHEMBL337820 | — | — | 1 | 8.00 |
| CHEMBL140706 | — | — | 1 | 7.96 |
| CHEMBL357557 | — | — | 1 | 7.96 |
| CHEMBL422326 | — | — | 1 | 7.96 |
| CHEMBL344607 | — | — | 1 | 7.92 |
| CHEMBL141699 | — | — | 1 | 7.75 |
| CHEMBL348667 | — | — | 1 | 7.70 |
| CHEMBL140490 | — | — | 1 | 7.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL140827 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL113436 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL334470 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL138502 | — | Ki | = | 5.23 | nM | 8.28 |
| CHEMBL322251 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL342137 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL337820 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL140706 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL357557 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL422326 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL344607 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL141699 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL348667 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL140490 | — | Ki | = | 38.0 | nM | 7.42 |