Assay Detail
Functional
CHEMBL1107996
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Antagonist activity at CXCR4 in human CEM-CCRF cells assessed as inhibition of SDF-1-induced calcium flux
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CEM-CCRF |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of novel small molecule orally bioavailable C-X-C chemokine receptor 4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.67 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1088913 | — | — | 1 | 7.96 |
| CHEMBL1093008 | — | — | 1 | 7.30 |
| CHEMBL1088912 | — | — | 1 | 7.17 |
| CHEMBL1088916 | — | — | 1 | 7.12 |
| CHEMBL1089844 | — | — | 1 | 7.11 |
| CHEMBL1092301 | — | — | 1 | 7.06 |
| CHEMBL1092324 | — | — | 1 | 6.92 |
| CHEMBL1089845 | — | — | 1 | 6.80 |
| CHEMBL1092302 | — | — | 1 | 6.72 |
| CHEMBL1092628 | — | — | 1 | 6.36 |
| CHEMBL1092596 | — | — | 1 | 6.29 |
| CHEMBL1089846 | — | — | 1 | 6.01 |
| CHEMBL1093302 | — | — | 1 | 5.86 |
| CHEMBL1088867 | — | — | 1 | 5.85 |
| CHEMBL1092629 | — | — | 1 | 5.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1088913 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1093008 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1088912 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL1088916 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL1089844 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL1092301 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL1092324 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL1089845 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1092302 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL1092628 | — | IC50 | = | 442.0 | nM | 6.36 |
| CHEMBL1092596 | — | IC50 | = | 514.0 | nM | 6.29 |
| CHEMBL1089846 | — | IC50 | = | 973.0 | nM | 6.01 |
| CHEMBL1093302 | — | IC50 | = | 1369.0 | nM | 5.86 |
| CHEMBL1088867 | — | IC50 | = | 1402.0 | nM | 5.85 |
| CHEMBL1092629 | — | IC50 | = | 3200.0 | nM | 5.50 |