Assay Detail
Functional
CHEMBL5154013
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at CCR5 (unknown origin) expressed in HEK293 cells co-expressing Galpha16 assessed as intracellular calcium change incubated for 15 mins by Fluo-4 AM calcium flux assay
23
Total Activities
23
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
Structure-Based Design of Tropane Derivatives as a Novel Series of CCR5 Antagonists with Broad-Spectrum Anti-HIV-1 Activities and Improved Oral Bioavailability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.64 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5171331 | — | — | 1 | 8.60 |
| CHEMBL5180628 | — | — | 1 | 8.36 |
| CHEMBL5177519 | — | — | 1 | 8.27 |
| CHEMBL256907 | MARAVIROC | 4.0 | 1 | 8.10 |
| CHEMBL5205216 | — | — | 1 | 8.10 |
| CHEMBL5209067 | — | — | 1 | 8.08 |
| CHEMBL5200961 | — | — | 1 | 8.03 |
| CHEMBL5185201 | — | — | 1 | 7.93 |
| CHEMBL5176665 | — | — | 1 | 7.82 |
| CHEMBL5175220 | — | — | 1 | 7.80 |
| CHEMBL5178121 | — | — | 1 | 7.72 |
| CHEMBL5203084 | — | — | 1 | 7.72 |
| CHEMBL5204027 | — | — | 1 | 7.67 |
| CHEMBL5197247 | — | — | 1 | 7.50 |
| CHEMBL5178495 | — | — | 1 | 7.39 |
| CHEMBL5208613 | — | — | 1 | 7.35 |
| CHEMBL4240742 | — | — | 1 | 7.17 |
| CHEMBL5205626 | — | — | 1 | 7.14 |
| CHEMBL5184527 | — | — | 1 | 6.17 |
| CHEMBL5184978 | — | — | 1 | 5.86 |
| CHEMBL5171807 | — | — | 1 | - |
| CHEMBL5194455 | — | — | 1 | - |
| CHEMBL5169473 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5171331 | — | IC50 | = | 2.49 | nM | 8.60 |
| CHEMBL5180628 | — | IC50 | = | 4.36 | nM | 8.36 |
| CHEMBL5177519 | — | IC50 | = | 5.34 | nM | 8.27 |
| CHEMBL256907 | MARAVIROC | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5205216 | — | IC50 | = | 7.99 | nM | 8.10 |
| CHEMBL5209067 | — | IC50 | = | 8.34 | nM | 8.08 |
| CHEMBL5200961 | — | IC50 | = | 9.33 | nM | 8.03 |
| CHEMBL5185201 | — | IC50 | = | 11.76 | nM | 7.93 |
| CHEMBL5176665 | — | IC50 | = | 15.04 | nM | 7.82 |
| CHEMBL5175220 | — | IC50 | = | 15.9 | nM | 7.80 |
| CHEMBL5178121 | — | IC50 | = | 18.91 | nM | 7.72 |
| CHEMBL5203084 | — | IC50 | = | 18.91 | nM | 7.72 |
| CHEMBL5204027 | — | IC50 | = | 21.46 | nM | 7.67 |
| CHEMBL5197247 | — | IC50 | = | 31.89 | nM | 7.50 |
| CHEMBL5178495 | — | IC50 | = | 40.4 | nM | 7.39 |
| CHEMBL5208613 | — | IC50 | = | 45.08 | nM | 7.35 |
| CHEMBL4240742 | — | IC50 | = | 67.39 | nM | 7.17 |
| CHEMBL5205626 | — | IC50 | = | 72.74 | nM | 7.14 |
| CHEMBL5184527 | — | IC50 | = | 680.2 | nM | 6.17 |
| CHEMBL5184978 | — | IC50 | = | 1381.0 | nM | 5.86 |
| CHEMBL5171807 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5194455 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5169473 | — | IC50 | > | 10000.0 | nM | - |