Assay Detail
Functional
CHEMBL4157559
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by Alamar blue assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | MDA-MB-231 |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
A Fragment-Derived Clinical Candidate for Antagonism of X-Linked and Cellular Inhibitor of Apoptosis Proteins: 1-(6-[(4-Fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-1 H,2 H,3 H-pyrrolo[3,2- b]pyridin-1-yl)-2-[(2 R,5 R)-5-methyl-2-([(3R)-3-methylmorpholin-4-yl]methyl)piperazin-1-yl]ethan-1-one (ASTX660).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 8.25 | 9.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4171490 | — | — | 1 | 9.23 |
| CHEMBL4166607 | — | — | 1 | 8.92 |
| CHEMBL4166057 | — | — | 1 | 8.74 |
| CHEMBL4173974 | ASTX-660 | 1.0 | 1 | 8.74 |
| CHEMBL4164271 | — | — | 1 | 8.72 |
| CHEMBL4167141 | — | — | 1 | 8.68 |
| CHEMBL4169478 | — | — | 1 | 8.62 |
| CHEMBL4174922 | — | — | 1 | 8.54 |
| CHEMBL4064619 | — | — | 1 | 8.36 |
| CHEMBL4167717 | — | — | 1 | 8.28 |
| CHEMBL4160872 | — | — | 1 | 8.27 |
| CHEMBL4168197 | — | — | 1 | 8.15 |
| CHEMBL2431768 | LCL-161 | 2.0 | 1 | 8.11 |
| CHEMBL4162607 | — | — | 1 | 8.10 |
| CHEMBL4175992 | — | — | 1 | 8.08 |
| CHEMBL4159232 | — | — | 1 | 7.96 |
| CHEMBL4159806 | — | — | 1 | 7.85 |
| CHEMBL4173890 | — | — | 1 | 7.85 |
| CHEMBL4170539 | — | — | 1 | 7.82 |
| CHEMBL4168144 | — | — | 1 | 7.80 |
| CHEMBL4177336 | — | — | 1 | 7.75 |
| CHEMBL4172596 | — | — | 1 | 7.66 |
| CHEMBL4159855 | — | — | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4171490 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL4166607 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4166057 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4173974 | ASTX-660 | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4164271 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4167141 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4169478 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4174922 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4064619 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL4167717 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL4160872 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4168197 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2431768 | LCL-161 | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4162607 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL4175992 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL4159232 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4159806 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4173890 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4170539 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4168144 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4177336 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4172596 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4159855 | — | IC50 | = | 26.0 | nM | 7.58 |