Assay Detail
Binding
CHEMBL4256813
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Displacement of AVPIAQKSEK-biotin from N-terminal His-tagged human recombinant XIAP BIR3 (253 to 347 residues) expressed in Escherichia coli BL21(DE3) Gold after 1 hr by DELFIA
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design of Potent pan-IAP and Lys-Covalent XIAP Selective Inhibitors Using a Thermodynamics Driven Approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.04 | 7.95 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4277819 | — | — | 1 | 7.95 |
| CHEMBL4281278 | — | — | 1 | 7.78 |
| CHEMBL4288451 | — | — | 1 | 7.63 |
| CHEMBL4291176 | — | — | 1 | 7.46 |
| CHEMBL4288478 | — | — | 1 | 7.43 |
| CHEMBL4283320 | — | — | 1 | 7.42 |
| CHEMBL4291896 | — | — | 1 | 7.33 |
| CHEMBL2063869 | GDC-0152 | 1.0 | 1 | 7.28 |
| CHEMBL4276715 | — | — | 1 | 7.11 |
| CHEMBL4277802 | — | — | 1 | 7.06 |
| CHEMBL4280168 | — | — | 1 | 6.97 |
| CHEMBL4288043 | — | — | 1 | 6.75 |
| CHEMBL4283597 | — | — | 1 | 6.72 |
| CHEMBL4276740 | — | — | 1 | 6.72 |
| CHEMBL4281250 | — | — | 1 | 6.67 |
| CHEMBL4291444 | — | — | 1 | 6.64 |
| CHEMBL4291873 | — | — | 1 | 6.56 |
| CHEMBL4284657 | — | — | 1 | 5.23 |
| CHEMBL4280144 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4277819 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL4281278 | — | IC50 | = | 16.6 | nM | 7.78 |
| CHEMBL4288451 | — | IC50 | = | 23.2 | nM | 7.63 |
| CHEMBL4291176 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4288478 | — | IC50 | = | 37.1 | nM | 7.43 |
| CHEMBL4283320 | — | IC50 | = | 38.3 | nM | 7.42 |
| CHEMBL4291896 | — | IC50 | = | 47.3 | nM | 7.33 |
| CHEMBL2063869 | GDC-0152 | IC50 | = | 52.7 | nM | 7.28 |
| CHEMBL4276715 | — | IC50 | = | 76.9 | nM | 7.11 |
| CHEMBL4277802 | — | IC50 | = | 86.8 | nM | 7.06 |
| CHEMBL4280168 | — | IC50 | = | 108.2 | nM | 6.97 |
| CHEMBL4288043 | — | IC50 | = | 175.9 | nM | 6.75 |
| CHEMBL4283597 | — | IC50 | = | 190.7 | nM | 6.72 |
| CHEMBL4276740 | — | IC50 | = | 189.4 | nM | 6.72 |
| CHEMBL4281250 | — | IC50 | = | 215.3 | nM | 6.67 |
| CHEMBL4291444 | — | IC50 | = | 229.4 | nM | 6.64 |
| CHEMBL4291873 | — | IC50 | = | 275.7 | nM | 6.56 |
| CHEMBL4284657 | — | IC50 | = | 5944.0 | nM | 5.23 |
| CHEMBL4280144 | — | IC50 | > | 10000.0 | nM | - |