Assay Detail
Binding
CHEMBL958140
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Displacement of [125I]CXCL12 from CXCR4 in rat IR983F cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | IR983F |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
C-X-C chemokine receptor type 4 (CHEMBL5556) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
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 | 4 | 7.01 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL460491 | — | — | 1 | 7.96 |
| CHEMBL452864 | — | — | 1 | 7.26 |
| CHEMBL18442 | PLERIXAFOR | 4.0 | 1 | 6.97 |
| CHEMBL506505 | — | — | 1 | 5.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL460491 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL452864 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL18442 | PLERIXAFOR | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL506505 | — | IC50 | = | 1440.0 | nM | 5.84 |