Assay Detail
Functional
CHEMBL4773458
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at CXCR4 in human CD4-positive T cells assessed as inhibition of CXCL12-induced cytosolic calcium flux preincubated for 20 mins followed by CXCL12 addition by calcium 4 dye based FLIPR TETRA analysis
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | T cell |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and evaluation of pyrrolidine based CXCR4 antagonists with in vivo anti-tumor metastatic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 8.69 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4799439 | — | — | 1 | 9.60 |
| CHEMBL4792975 | — | — | 1 | 9.40 |
| CHEMBL4799191 | — | — | 1 | 8.96 |
| CHEMBL4777386 | — | — | 1 | 8.74 |
| CHEMBL4783831 | — | — | 1 | 8.57 |
| CHEMBL4789233 | — | — | 1 | 8.57 |
| CHEMBL4795444 | — | — | 1 | 8.31 |
| CHEMBL18442 | PLERIXAFOR | 4.0 | 1 | 8.21 |
| CHEMBL4787045 | — | — | 1 | 7.89 |
| CHEMBL4797343 | — | — | 1 | - |
| CHEMBL4783241 | — | — | 1 | - |
| CHEMBL4785166 | — | — | 1 | - |
| CHEMBL4777987 | — | — | 1 | - |
| CHEMBL4794732 | — | — | 1 | - |
| CHEMBL4795219 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4799439 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL4792975 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4799191 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4777386 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4783831 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4789233 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4795444 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL18442 | PLERIXAFOR | IC50 | = | 6.134 | nM | 8.21 |
| CHEMBL4787045 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4797343 | — | IC50 | - | — | - | |
| CHEMBL4783241 | — | IC50 | - | — | - | |
| CHEMBL4785166 | — | IC50 | - | — | - | |
| CHEMBL4777987 | — | IC50 | - | — | - | |
| CHEMBL4794732 | — | IC50 | - | — | - | |
| CHEMBL4795219 | — | IC50 | - | — | - |