Assay Detail
Binding
CHEMBL649956
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Binding affinity towards C-C chemokine receptor type 5
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. II. Discovery of 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4- methyl-4-[3(S)-methyl-4-[1(S)-[4-(trifluoromethyl)phenyl]ethyl]-1-piperazinyl]- piperidine N1-oxide (Sch-350634), an orally bioavailable, potent CCR5 antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.91 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL113072 | — | — | 1 | 8.52 |
| CHEMBL113042 | — | — | 1 | 8.30 |
| CHEMBL325276 | — | — | 1 | 8.30 |
| CHEMBL115716 | — | — | 1 | 8.30 |
| CHEMBL113154 | — | — | 1 | 8.30 |
| CHEMBL111998 | — | — | 1 | 8.30 |
| CHEMBL115487 | — | — | 1 | 8.15 |
| CHEMBL325556 | — | — | 1 | 8.10 |
| CHEMBL326020 | — | — | 1 | 7.92 |
| CHEMBL112299 | — | — | 1 | 7.82 |
| CHEMBL112659 | — | — | 1 | 7.70 |
| CHEMBL322817 | — | — | 1 | 7.64 |
| CHEMBL116008 | — | — | 1 | 7.52 |
| CHEMBL113648 | — | — | 1 | 7.21 |
| CHEMBL325957 | — | — | 1 | 6.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL113072 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL113042 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL325276 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL115716 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL113154 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL111998 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL115487 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL325556 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL326020 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL112299 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL112659 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL322817 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL116008 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL113648 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL325957 | — | Ki | = | 275.0 | nM | 6.56 |