Assay Detail
Binding
CHEMBL4157561
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Induction of intracellular cIAP1 degradation in human MDA-MB-231 cells after 2 hrs
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDA-MB-231 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Baculoviral IAP repeat-containing protein 2 (CHEMBL5462) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 9.17 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4166057 | — | — | 1 | 10.00 |
| CHEMBL4167141 | — | — | 1 | 9.89 |
| CHEMBL4171490 | — | — | 1 | 9.77 |
| CHEMBL4169478 | — | — | 1 | 9.74 |
| CHEMBL4166607 | — | — | 1 | 9.72 |
| CHEMBL4164271 | — | — | 1 | 9.70 |
| CHEMBL4173974 | ASTX-660 | 1.0 | 1 | 9.66 |
| CHEMBL4064619 | — | — | 1 | 9.49 |
| CHEMBL4160872 | — | — | 1 | 9.47 |
| CHEMBL2431768 | LCL-161 | 2.0 | 1 | 9.40 |
| CHEMBL4159232 | — | — | 1 | 9.23 |
| CHEMBL4168197 | — | — | 1 | 9.21 |
| CHEMBL4177336 | — | — | 1 | 9.15 |
| CHEMBL4174922 | — | — | 1 | 9.13 |
| CHEMBL4167717 | — | — | 1 | 9.00 |
| CHEMBL4175992 | — | — | 1 | 8.89 |
| CHEMBL4159806 | — | — | 1 | 8.80 |
| CHEMBL4162607 | — | — | 1 | 8.64 |
| CHEMBL4168144 | — | — | 1 | 8.60 |
| CHEMBL4170539 | — | — | 1 | 8.46 |
| CHEMBL4173890 | — | — | 1 | 8.42 |
| CHEMBL4159855 | — | — | 1 | 8.38 |
| CHEMBL4172596 | — | — | 1 | 8.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4166057 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4167141 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL4171490 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL4169478 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL4166607 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL4164271 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4173974 | ASTX-660 | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL4064619 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL4160872 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL2431768 | LCL-161 | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4159232 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL4168197 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL4177336 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4174922 | — | IC50 | = | 0.74 | nM | 9.13 |
| CHEMBL4167717 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4175992 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4159806 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4162607 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4168144 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4170539 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4173890 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4159855 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4172596 | — | IC50 | = | 6.5 | nM | 8.19 |