Assay Detail
Binding
CHEMBL2406570
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Competitive inhibition of XIAP-BIR3 domain (unknown origin) by fluorescence polarization assay
29
Total Activities
29
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, synthesis and evaluation of inhibitor of apoptosis protein (IAP) antagonists that are highly selective for the BIR2 domain of XIAP.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 5.37 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1621842 | — | — | 1 | 7.22 |
| CHEMBL2063869 | GDC-0152 | 1.0 | 1 | 6.58 |
| CHEMBL2403872 | — | — | 1 | 6.54 |
| CHEMBL2401764 | — | — | 1 | 6.28 |
| CHEMBL2401761 | — | — | 1 | 6.17 |
| CHEMBL2403871 | — | — | 1 | 6.11 |
| CHEMBL1625066 | — | — | 1 | 5.97 |
| CHEMBL2401762 | — | — | 1 | 5.95 |
| CHEMBL1624713 | — | — | 1 | 5.82 |
| CHEMBL2403873 | — | — | 1 | 5.70 |
| CHEMBL2401763 | — | — | 1 | 5.69 |
| CHEMBL1627154 | — | — | 1 | 5.06 |
| CHEMBL1618815 | — | — | 1 | 5.01 |
| CHEMBL1618558 | — | — | 1 | 4.67 |
| CHEMBL1622095 | — | — | 1 | 4.67 |
| CHEMBL2401765 | — | — | 1 | 4.52 |
| CHEMBL1621070 | — | — | 1 | 4.47 |
| CHEMBL1623606 | — | — | 1 | 4.41 |
| CHEMBL1617615 | — | — | 1 | 4.40 |
| CHEMBL1617819 | — | — | 1 | 4.38 |
| CHEMBL1626340 | — | — | 1 | 4.29 |
| CHEMBL1625435 | — | — | 1 | 4.18 |
| CHEMBL1619873 | — | — | 1 | - |
| CHEMBL1620115 | — | — | 1 | - |
| CHEMBL1616141 | — | — | 1 | - |
| CHEMBL1625863 | — | — | 1 | - |
| CHEMBL1617821 | — | — | 1 | - |
| CHEMBL2401766 | — | — | 1 | - |
| CHEMBL1624542 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1621842 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL2063869 | GDC-0152 | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL2403872 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL2401764 | — | Ki | = | 530.0 | nM | 6.28 |
| CHEMBL2401761 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL2403871 | — | Ki | = | 780.0 | nM | 6.11 |
| CHEMBL1625066 | — | Ki | = | 1080.0 | nM | 5.97 |
| CHEMBL2401762 | — | Ki | = | 1130.0 | nM | 5.95 |
| CHEMBL1624713 | — | Ki | = | 1510.0 | nM | 5.82 |
| CHEMBL2403873 | — | Ki | = | 2020.0 | nM | 5.70 |
| CHEMBL2401763 | — | Ki | = | 2050.0 | nM | 5.69 |
| CHEMBL1627154 | — | Ki | = | 8790.0 | nM | 5.06 |
| CHEMBL1618815 | — | Ki | = | 9820.0 | nM | 5.01 |
| CHEMBL1618558 | — | Ki | = | 21150.0 | nM | 4.67 |
| CHEMBL1622095 | — | Ki | = | 21480.0 | nM | 4.67 |
| CHEMBL2401765 | — | Ki | = | 30070.0 | nM | 4.52 |
| CHEMBL1621070 | — | Ki | = | 34180.0 | nM | 4.47 |
| CHEMBL1623606 | — | Ki | = | 39000.0 | nM | 4.41 |
| CHEMBL1617615 | — | Ki | = | 40150.0 | nM | 4.40 |
| CHEMBL1617819 | — | Ki | = | 41320.0 | nM | 4.38 |
| CHEMBL1626340 | — | Ki | = | 51790.0 | nM | 4.29 |
| CHEMBL1625435 | — | Ki | = | 65620.0 | nM | 4.18 |
| CHEMBL1619873 | — | Ki | > | 39000.0 | nM | - |
| CHEMBL1620115 | — | Ki | > | 39000.0 | nM | - |
| CHEMBL1616141 | — | Ki | > | 39000.0 | nM | - |
| CHEMBL1625863 | — | Ki | > | 39000.0 | nM | - |
| CHEMBL1617821 | — | Ki | > | 39000.0 | nM | - |
| CHEMBL2401766 | — | Ki | > | 39000.0 | nM | - |
| CHEMBL1624542 | — | Ki | > | 39000.0 | nM | - |