Assay Detail
Functional
CHEMBL4149799
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 SDS1alpha-induced calcium flux pretreated for 25 mins followed by SDS1alpha addition measured for 90 secs by calcium-dye based assay
22
Total Activities
22
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
Discovery of N-Alkyl Piperazine Side Chain Based CXCR4 Antagonists with Improved Drug-like Properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.92 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL518924 | MAVORIXAFOR | 4.0 | 1 | 8.30 |
| CHEMBL3091687 | — | — | 1 | 8.22 |
| CHEMBL4174290 | — | — | 1 | 7.80 |
| CHEMBL4167058 | — | — | 1 | 7.77 |
| CHEMBL4172802 | — | — | 1 | 7.77 |
| CHEMBL4175653 | — | — | 1 | 7.48 |
| CHEMBL4161613 | — | — | 1 | 7.35 |
| CHEMBL4167654 | — | — | 1 | 7.30 |
| CHEMBL4159991 | — | — | 1 | 7.21 |
| CHEMBL4159410 | — | — | 1 | 7.19 |
| CHEMBL4159150 | — | — | 1 | 7.18 |
| CHEMBL4165032 | — | — | 1 | 6.90 |
| CHEMBL4164702 | — | — | 1 | 6.82 |
| CHEMBL4163611 | — | — | 1 | 6.79 |
| CHEMBL4175350 | — | — | 1 | 6.77 |
| CHEMBL4170141 | — | — | 1 | 6.27 |
| CHEMBL4166456 | — | — | 1 | 6.26 |
| CHEMBL4160551 | — | — | 1 | 6.02 |
| CHEMBL4170857 | — | — | 1 | 5.94 |
| CHEMBL4172234 | — | — | 1 | 5.92 |
| CHEMBL4167467 | — | — | 1 | 5.58 |
| CHEMBL4162125 | — | — | 1 | 5.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL518924 | MAVORIXAFOR | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3091687 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4174290 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4167058 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4172802 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4175653 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4161613 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4167654 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4159991 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4159410 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4159150 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4165032 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL4164702 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4163611 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL4175350 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL4170141 | — | IC50 | = | 536.0 | nM | 6.27 |
| CHEMBL4166456 | — | IC50 | = | 553.0 | nM | 6.26 |
| CHEMBL4160551 | — | IC50 | = | 959.0 | nM | 6.02 |
| CHEMBL4170857 | — | IC50 | = | 1154.0 | nM | 5.94 |
| CHEMBL4172234 | — | IC50 | = | 1199.0 | nM | 5.92 |
| CHEMBL4167467 | — | IC50 | = | 2639.0 | nM | 5.58 |
| CHEMBL4162125 | — | IC50 | = | 4316.0 | nM | 5.37 |