Assay Detail
Functional
CHEMBL4384563
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human DEF3-fused CXCR4 receptor expressed in HEK293T cells co-expressing DAN1-HA-Galphaq/i5 assessed as inhibition of CXCL12-induced IP3 accumulation after 90 mins in presence of [3H]-myo-inositol by scintillation counting analysis
8
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 | 6.23 | 7.30 |
| Inhibition | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL460491 | — | — | 1 | 7.30 |
| CHEMBL4452433 | — | — | 2 | 6.00 |
| CHEMBL4438964 | — | — | 2 | 5.90 |
| CHEMBL4514484 | — | — | 2 | 5.70 |
| CHEMBL4531030 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL460491 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL4452433 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4438964 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL4514484 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL4452433 | — | Inhibition | - | % | - | |
| CHEMBL4438964 | — | Inhibition | - | % | - | |
| CHEMBL4514484 | — | Inhibition | - | % | - | |
| CHEMBL4531030 | — | IC50 | > | 31622.78 | nM | - |