Assay Detail
Binding
CHEMBL1108788
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kalpha after 15 to 30 mins by fluorescence polarization assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (CHEMBL4005) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: optimization of human microsomal stability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 6.42 | 7.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1091714 | — | — | 1 | 7.37 |
| CHEMBL1091349 | — | — | 1 | 7.29 |
| CHEMBL1092389 | — | — | 1 | 7.28 |
| CHEMBL1091358 | — | — | 1 | 7.27 |
| CHEMBL1092390 | — | — | 1 | 7.22 |
| CHEMBL1091357 | — | — | 1 | 7.11 |
| CHEMBL1091355 | — | — | 1 | 7.10 |
| CHEMBL1091713 | — | — | 1 | 6.99 |
| CHEMBL1091356 | — | — | 1 | 6.83 |
| CHEMBL1092394 | — | — | 1 | 6.65 |
| CHEMBL1091596 | — | — | 1 | 6.60 |
| CHEMBL1091360 | — | — | 1 | 6.54 |
| CHEMBL1091351 | — | — | 1 | 6.53 |
| CHEMBL1091354 | — | — | 1 | 6.42 |
| CHEMBL1092397 | — | — | 1 | 6.41 |
| CHEMBL1091712 | — | — | 1 | 6.35 |
| CHEMBL1092396 | — | — | 1 | 6.32 |
| CHEMBL1092393 | — | — | 1 | 6.30 |
| CHEMBL1091352 | — | — | 1 | 6.24 |
| CHEMBL1091347 | — | — | 1 | 6.23 |
| CHEMBL1091715 | — | — | 1 | 6.21 |
| CHEMBL1091353 | — | — | 1 | 6.18 |
| CHEMBL1091348 | — | — | 1 | 6.18 |
| CHEMBL1091350 | — | — | 1 | 6.11 |
| CHEMBL1091359 | — | — | 1 | 6.06 |
| CHEMBL1088973 | — | — | 1 | 6.05 |
| CHEMBL1092398 | — | — | 1 | 6.02 |
| CHEMBL1092395 | — | — | 1 | 6.02 |
| CHEMBL1092391 | — | — | 1 | 6.02 |
| CHEMBL1091711 | — | — | 1 | 6.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1091714 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL1091349 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL1092389 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL1091358 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL1092390 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1091357 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL1091355 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL1091713 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL1091356 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL1092394 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL1091596 | — | IC50 | = | 253.0 | nM | 6.60 |
| CHEMBL1091360 | — | IC50 | = | 286.0 | nM | 6.54 |
| CHEMBL1091351 | — | IC50 | = | 294.0 | nM | 6.53 |
| CHEMBL1091354 | — | IC50 | = | 382.0 | nM | 6.42 |
| CHEMBL1092397 | — | IC50 | = | 389.0 | nM | 6.41 |
| CHEMBL1091712 | — | IC50 | = | 443.0 | nM | 6.35 |
| CHEMBL1092396 | — | IC50 | = | 483.0 | nM | 6.32 |
| CHEMBL1092393 | — | IC50 | = | 499.0 | nM | 6.30 |
| CHEMBL1091352 | — | IC50 | = | 574.0 | nM | 6.24 |
| CHEMBL1091347 | — | IC50 | = | 592.0 | nM | 6.23 |
| CHEMBL1091715 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL1091353 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL1091348 | — | IC50 | = | 665.0 | nM | 6.18 |
| CHEMBL1091350 | — | IC50 | = | 777.0 | nM | 6.11 |
| CHEMBL1091359 | — | IC50 | = | 876.0 | nM | 6.06 |
| CHEMBL1088973 | — | IC50 | = | 899.0 | nM | 6.05 |
| CHEMBL1092398 | — | IC50 | = | 961.0 | nM | 6.02 |
| CHEMBL1092391 | — | IC50 | = | 947.0 | nM | 6.02 |
| CHEMBL1092395 | — | IC50 | = | 955.0 | nM | 6.02 |
| CHEMBL1091711 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL1076864 | — | IC50 | = | 1006.0 | nM | 6.00 |
| CHEMBL1091344 | — | IC50 | = | 1028.0 | nM | 5.99 |
| CHEMBL1092392 | — | IC50 | = | 1127.0 | nM | 5.95 |
| CHEMBL1091345 | — | IC50 | = | 2506.0 | nM | 5.60 |
| CHEMBL1091346 | — | IC50 | = | 4766.0 | nM | 5.32 |