Assay Detail
Functional
CHEMBL951599
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Antagonist activity at human CXCR4 I284A 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 | 6.37 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL477121 | — | — | 2 | 7.52 |
| CHEMBL478168 | — | — | 2 | 6.38 |
| CHEMBL18442 | PLERIXAFOR | 4.0 | 2 | 5.92 |
| CHEMBL122226 | — | — | 2 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL477121 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL478168 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL18442 | PLERIXAFOR | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL122226 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL18442 | PLERIXAFOR | logIC50 | = | -5.94 | — | - |
| CHEMBL122226 | — | logIC50 | = | -5.64 | — | - |
| CHEMBL478168 | — | logIC50 | = | -6.38 | — | - |
| CHEMBL477121 | — | logIC50 | = | -7.5 | — | - |