Assay Detail
Functional
CHEMBL4144845
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at CXCR4 in human CCRF-CEM cells assessed as inhibition of CXCL12-mediated calcium flux incubated for 25 mins followed by CXCL12 stimulation measured for 90 secs
17
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CCRF-CEM |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis of Novel Tetrahydroisoquinoline CXCR4 Antagonists with Rigidified Side-Chains.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.11 | 8.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4163770 | — | — | 2 | 8.19 |
| CHEMBL4159607 | — | — | 1 | 8.07 |
| CHEMBL4096305 | — | — | 1 | 8.00 |
| CHEMBL4164075 | — | — | 1 | 7.55 |
| CHEMBL4161528 | — | — | 1 | 7.55 |
| CHEMBL4175088 | — | — | 1 | 7.47 |
| CHEMBL4175500 | — | — | 1 | 7.36 |
| CHEMBL4174727 | — | — | 1 | 7.10 |
| CHEMBL4164874 | — | — | 1 | 7.01 |
| CHEMBL4086147 | — | — | 1 | 6.89 |
| CHEMBL4160401 | — | — | 1 | 6.68 |
| CHEMBL4167521 | — | — | 1 | 6.64 |
| CHEMBL4171643 | — | — | 1 | 6.55 |
| CHEMBL4167221 | — | — | 1 | 6.47 |
| CHEMBL4169450 | — | — | 1 | 5.75 |
| CHEMBL4161850 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4163770 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4159607 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL4096305 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4163770 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4164075 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4161528 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4175088 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4175500 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4174727 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4164874 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4086147 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4160401 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4167521 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4171643 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4167221 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4169450 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4161850 | — | IC50 | = | 1800.0 | nM | 5.75 |