Assay Detail
Binding
CHEMBL4339724
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Antagonist activity at CCR5 (unknown origin) expressed in human HT1080 cells assessed as blockade of MIP1beta-binding to receptor
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Use of a Conformational-Switching Mechanism to Modulate Exposed Polarity: Discovery of CCR2 Antagonist BMS-741672.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.43 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3577945 | — | — | 1 | 8.62 |
| CHEMBL4470701 | — | — | 1 | 6.72 |
| CHEMBL4457723 | BMS-741672 | 2.0 | 1 | 6.54 |
| CHEMBL4442783 | — | — | 1 | 6.11 |
| CHEMBL4465351 | — | — | 1 | 5.80 |
| CHEMBL3233178 | — | — | 1 | 5.79 |
| CHEMBL4463290 | — | — | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3577945 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4470701 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4457723 | BMS-741672 | IC50 | = | 287.0 | nM | 6.54 |
| CHEMBL4442783 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL4465351 | — | IC50 | = | 1570.0 | nM | 5.80 |
| CHEMBL3233178 | — | IC50 | = | 1636.0 | nM | 5.79 |
| CHEMBL4463290 | — | IC50 | = | 3469.0 | nM | 5.46 |