Assay Detail
Functional
CHEMBL4845505
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at CXCR4 receptor in human CCRF-CEM cells assessed as inhibition of SDF-1alpha-induced calcium release preincubated for 25 mins followed by SDF-1alpha addition and monitered for 90 sec
15
Total Activities
15
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
Amino-Heterocycle Tetrahydroisoquinoline CXCR4 Antagonists with Improved ADME Profiles via Late-Stage Buchwald Couplings.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.59 | 8.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL518924 | MAVORIXAFOR | 4.0 | 1 | 8.29 |
| CHEMBL3091687 | — | — | 1 | 8.20 |
| CHEMBL4862509 | — | — | 1 | 8.02 |
| CHEMBL4853570 | — | — | 1 | 7.99 |
| CHEMBL4877757 | — | — | 1 | 7.98 |
| CHEMBL4863276 | — | — | 1 | 7.96 |
| CHEMBL4875030 | — | — | 1 | 7.94 |
| CHEMBL4857452 | — | — | 1 | 7.87 |
| CHEMBL4874526 | — | — | 1 | 7.74 |
| CHEMBL4862362 | — | — | 1 | 7.73 |
| CHEMBL4846946 | — | — | 1 | 7.48 |
| CHEMBL4876951 | — | — | 1 | 7.45 |
| CHEMBL4858136 | — | — | 1 | 7.32 |
| CHEMBL4864332 | — | — | 1 | 6.12 |
| CHEMBL4849088 | — | — | 1 | 5.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL518924 | MAVORIXAFOR | IC50 | = | 5.18 | nM | 8.29 |
| CHEMBL3091687 | — | IC50 | = | 6.25 | nM | 8.20 |
| CHEMBL4862509 | — | IC50 | = | 9.56 | nM | 8.02 |
| CHEMBL4853570 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL4877757 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL4863276 | — | IC50 | = | 10.9 | nM | 7.96 |
| CHEMBL4875030 | — | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL4857452 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL4874526 | — | IC50 | = | 18.1 | nM | 7.74 |
| CHEMBL4862362 | — | IC50 | = | 18.7 | nM | 7.73 |
| CHEMBL4846946 | — | IC50 | = | 33.4 | nM | 7.48 |
| CHEMBL4876951 | — | IC50 | = | 35.9 | nM | 7.45 |
| CHEMBL4858136 | — | IC50 | = | 47.4 | nM | 7.32 |
| CHEMBL4864332 | — | IC50 | = | 755.0 | nM | 6.12 |
| CHEMBL4849088 | — | IC50 | = | 1670.0 | nM | 5.78 |