Assay Detail
Functional
CHEMBL951598
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Antagonist activity at human CXCR4 H281A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover
8
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Molecular mechanism of action of monocyclam versus bicyclam non-peptide antagonists in the CXCR4 chemokine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| logIC50 | 4 | - | - |
| Ki | 4 | 5.73 | 6.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL18442 | PLERIXAFOR | 4.0 | 2 | 6.72 |
| CHEMBL477121 | — | — | 2 | 5.80 |
| CHEMBL478168 | — | — | 2 | 5.75 |
| CHEMBL122226 | — | — | 2 | 4.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL18442 | PLERIXAFOR | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL477121 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL478168 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL122226 | — | Ki | = | 22000.0 | nM | 4.66 |
| CHEMBL18442 | PLERIXAFOR | logIC50 | = | -6.73 | — | - |
| CHEMBL122226 | — | logIC50 | = | 4.66 | — | - |
| CHEMBL478168 | — | logIC50 | = | -5.75 | — | - |
| CHEMBL477121 | — | logIC50 | = | -5.8 | — | - |