Assay Detail
Functional
CHEMBL5031207
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Antagonist activity at human CCR5 receptor expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of RNATES-induced intracellular calcium flux measured after 10 mins by FLIPR calcium mobilization assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
A "Two-Birds-One-Stone" Approach toward the Design of Bifunctional Human Immunodeficiency Virus Type 1 Entry Inhibitors Targeting the CCR5 Coreceptor and gp41 N-Terminal Heptad Repeat Region.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.39 | 9.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL256907 | MARAVIROC | 4.0 | 1 | 9.09 |
| CHEMBL5084989 | — | — | 1 | 8.83 |
| CHEMBL5078769 | — | — | 1 | 7.26 |
| CHEMBL5075904 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL256907 | MARAVIROC | IC50 | = | 0.82 | nM | 9.09 |
| CHEMBL5084989 | — | IC50 | = | 1.49 | nM | 8.83 |
| CHEMBL5078769 | — | IC50 | = | 55.47 | nM | 7.26 |
| CHEMBL5075904 | — | IC50 | > | 10000.0 | nM | - |