Assay Detail
Functional
CHEMBL1685195
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Antagonist activity at CXCR4 in human CEM-CCRF cells assessed as inhibition of SDF-1-induced calcium signaling
22
Total Activities
22
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
Design of novel CXCR4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.28 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1682993 | — | — | 1 | 8.10 |
| CHEMBL1682854 | — | — | 1 | 7.75 |
| CHEMBL1682989 | — | — | 1 | 7.75 |
| CHEMBL1682859 | — | — | 1 | 7.72 |
| CHEMBL1682992 | — | — | 1 | 7.70 |
| CHEMBL1682986 | — | — | 1 | 7.64 |
| CHEMBL1682863 | — | — | 1 | 7.57 |
| CHEMBL1682856 | — | — | 1 | 7.46 |
| CHEMBL1682858 | — | — | 1 | 7.42 |
| CHEMBL1682866 | — | — | 1 | 7.36 |
| CHEMBL1682860 | — | — | 1 | 7.31 |
| CHEMBL1682857 | — | — | 1 | 7.28 |
| CHEMBL1682864 | — | — | 1 | 7.20 |
| CHEMBL1682990 | — | — | 1 | 7.18 |
| CHEMBL1682987 | — | — | 1 | 7.14 |
| CHEMBL1099015 | — | — | 1 | 7.13 |
| CHEMBL1682865 | — | — | 1 | 7.10 |
| CHEMBL1682855 | — | — | 1 | 7.04 |
| CHEMBL1682988 | — | — | 1 | 6.96 |
| CHEMBL1682862 | — | — | 1 | 6.89 |
| CHEMBL1682991 | — | — | 1 | 6.74 |
| CHEMBL1682861 | — | — | 1 | 5.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1682993 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1682854 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1682989 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1682859 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1682992 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1682986 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1682863 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1682856 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1682858 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL1682866 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL1682860 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL1682857 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL1682864 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL1682990 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL1682987 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL1099015 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL1682865 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL1682855 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL1682988 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL1682862 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL1682991 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL1682861 | — | IC50 | = | 1621.0 | nM | 5.79 |