Assay Detail
Binding
CHEMBL4384561
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human DEF3-RLuc fused CXCR4 receptor expressed in HEK293T cells co-expressing DEF3-Beta-arrestin-2-mVenus assessed as inhibition of CXCL12-induced beta-arrestin2 recruitment preincubated for 60 mins followed by CXCL12 addition measured after 20 mins by BRET assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-based exploration and pharmacological evaluation of N-substituted piperidin-4-yl-methanamine CXCR4 chemokine receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.95 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL460491 | — | — | 1 | 7.30 |
| CHEMBL4438964 | — | — | 1 | 5.60 |
| CHEMBL4452433 | — | — | 1 | 5.50 |
| CHEMBL4514484 | — | — | 1 | 5.40 |
| CHEMBL4531030 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL460491 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL4438964 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL4452433 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL4514484 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL4531030 | — | IC50 | > | 31622.78 | nM | - |