Assay Detail
Functional
CHEMBL958141
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Activity at CXCR4 in human CEM cells assessed as inhibition of CXCL12-induced calcium mobilization
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CCRF-CEM |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Orally bioavailable isothioureas block function of the chemokine receptor CXCR4 in vitro and in vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.05 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL460491 | — | — | 1 | 8.96 |
| CHEMBL518501 | — | — | 1 | 8.68 |
| CHEMBL508054 | — | — | 1 | 8.51 |
| CHEMBL454896 | — | — | 1 | 8.28 |
| CHEMBL541728 | — | — | 1 | 8.18 |
| CHEMBL460298 | — | — | 1 | 8.10 |
| CHEMBL452864 | — | — | 1 | 7.96 |
| CHEMBL461359 | — | — | 1 | 7.89 |
| CHEMBL516630 | — | — | 1 | 7.24 |
| CHEMBL461358 | — | — | 1 | 7.12 |
| CHEMBL460299 | — | — | 1 | 6.76 |
| CHEMBL518041 | — | — | 1 | 6.52 |
| CHEMBL462588 | — | — | 1 | 6.36 |
| CHEMBL454689 | — | — | 1 | 6.31 |
| CHEMBL452868 | — | — | 1 | 6.03 |
| CHEMBL516480 | — | — | 1 | 5.65 |
| CHEMBL460482 | — | — | 1 | 5.28 |
| CHEMBL516989 | — | — | 1 | 5.09 |
| CHEMBL460484 | — | — | 1 | 5.04 |
| CHEMBL460483 | — | — | 1 | - |
| CHEMBL455708 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL460491 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL518501 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL508054 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL454896 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL541728 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL460298 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL452864 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL461359 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL516630 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL461358 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL460299 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL518041 | — | IC50 | = | 304.0 | nM | 6.52 |
| CHEMBL462588 | — | IC50 | = | 437.0 | nM | 6.36 |
| CHEMBL454689 | — | IC50 | = | 493.0 | nM | 6.31 |
| CHEMBL452868 | — | IC50 | = | 931.0 | nM | 6.03 |
| CHEMBL516480 | — | IC50 | = | 2220.0 | nM | 5.65 |
| CHEMBL460482 | — | IC50 | = | 5275.0 | nM | 5.28 |
| CHEMBL516989 | — | IC50 | = | 8120.0 | nM | 5.09 |
| CHEMBL460484 | — | IC50 | = | 9130.0 | nM | 5.04 |
| CHEMBL460483 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL455708 | — | IC50 | - | — | - |