Assay Detail
Binding
CHEMBL4157560
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Inhibition of full length FLAG-tagged XIAP (unknown origin) interaction with full length untagged caspase-9 expressed in HEK293 cells after 2 hrs by immunoprecipitation assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
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 | 8.04 | 9.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4169478 | — | — | 1 | 9.08 |
| CHEMBL4166057 | — | — | 1 | 8.80 |
| CHEMBL4173974 | ASTX-660 | 1.0 | 1 | 8.55 |
| CHEMBL4166607 | — | — | 1 | 8.54 |
| CHEMBL4164271 | — | — | 1 | 8.46 |
| CHEMBL4171490 | — | — | 1 | 8.37 |
| CHEMBL4064619 | — | — | 1 | 8.29 |
| CHEMBL4167141 | — | — | 1 | 8.27 |
| CHEMBL4159806 | — | — | 1 | 8.24 |
| CHEMBL4170539 | — | — | 1 | 8.13 |
| CHEMBL4174922 | — | — | 1 | 8.12 |
| CHEMBL4160872 | — | — | 1 | 7.92 |
| CHEMBL4177336 | — | — | 1 | 7.85 |
| CHEMBL4168197 | — | — | 1 | 7.85 |
| CHEMBL4172596 | — | — | 1 | 7.85 |
| CHEMBL4167717 | — | — | 1 | 7.80 |
| CHEMBL4159232 | — | — | 1 | 7.77 |
| CHEMBL4173890 | — | — | 1 | 7.75 |
| CHEMBL4159855 | — | — | 1 | 7.70 |
| CHEMBL4175992 | — | — | 1 | 7.52 |
| CHEMBL2431768 | LCL-161 | 2.0 | 1 | 7.46 |
| CHEMBL4168144 | — | — | 1 | 7.33 |
| CHEMBL4162607 | — | — | 1 | 7.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4169478 | — | IC50 | = | 0.83 | nM | 9.08 |
| CHEMBL4166057 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4173974 | ASTX-660 | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4166607 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4164271 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4171490 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4064619 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4167141 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4159806 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL4170539 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL4174922 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL4160872 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4177336 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4168197 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4172596 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4167717 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4159232 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4173890 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4159855 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4175992 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2431768 | LCL-161 | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4168144 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4162607 | — | IC50 | = | 47.0 | nM | 7.33 |