Assay Detail
Functional
CHEMBL3097226
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Antagonist activity at CXCR4 in human Chem-1 cells assessed as inhibition of SDF-1alpha-mediated calcium flux preincubated for 10 mins by FLIPR assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Chem-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of tetrahydroisoquinoline-based CXCR4 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.44 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3091683 | — | — | 1 | 9.00 |
| CHEMBL3091685 | — | — | 1 | 8.52 |
| CHEMBL3091687 | — | — | 1 | 8.52 |
| CHEMBL3091684 | — | — | 1 | 8.40 |
| CHEMBL3091682 | — | — | 1 | 8.15 |
| CHEMBL3091681 | — | — | 1 | 8.10 |
| CHEMBL3091693 | — | — | 1 | 7.41 |
| CHEMBL3091688 | — | — | 1 | 7.25 |
| CHEMBL3091694 | — | — | 1 | 6.85 |
| CHEMBL3091686 | — | — | 1 | 6.75 |
| CHEMBL3091689 | — | — | 1 | 6.46 |
| CHEMBL3091691 | — | — | 1 | 6.31 |
| CHEMBL3091692 | — | — | 1 | 6.24 |
| CHEMBL3091690 | — | — | 1 | 6.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3091683 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3091685 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3091687 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3091684 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3091682 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3091681 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3091693 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3091688 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL3091694 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3091686 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3091689 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3091691 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL3091692 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL3091690 | — | IC50 | = | 660.0 | nM | 6.18 |