Assay Detail
Binding
CHEMBL869753
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Inhibition of radio-isotope labeled MIP1-alpha binding to human recombinant CCR5
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Design, synthesis, and biological evaluation of the combinatorial library with a new spirodiketopiperazine scaffold. Discovery of novel potent and selective low-molecular-weight CCR5 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.42 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL556798 | — | — | 1 | 8.60 |
| CHEMBL557015 | — | — | 1 | 8.35 |
| CHEMBL536743 | — | — | 1 | 8.21 |
| CHEMBL540108 | — | — | 1 | 7.96 |
| CHEMBL557150 | — | — | 1 | 7.77 |
| CHEMBL540366 | — | — | 1 | 7.70 |
| CHEMBL536288 | — | — | 1 | 7.42 |
| CHEMBL537424 | — | — | 1 | 7.08 |
| CHEMBL557199 | — | — | 1 | 6.25 |
| CHEMBL538084 | — | — | 1 | 6.21 |
| CHEMBL537425 | — | — | 1 | 6.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL556798 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL557015 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL536743 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL540108 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL557150 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL540366 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL536288 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL537424 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL557199 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL538084 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL537425 | — | IC50 | = | 860.0 | nM | 6.07 |