Assay Detail
Binding
CHEMBL5138979
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kalpha in rat Rat1 cells assessed as reduction in phosphorylation of AKT at Ser473 residue incubated for 1 hr by cellular assay
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | Rat1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (CHEMBL5169092) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 6.62 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1879463 | DACTOLISIB | 3.0 | 1 | 8.28 |
| CHEMBL5174001 | — | — | 1 | 7.41 |
| CHEMBL5203121 | — | — | 1 | 7.38 |
| CHEMBL5177354 | — | — | 1 | 7.32 |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 7.28 |
| CHEMBL2017976 | — | — | 1 | 7.20 |
| CHEMBL5188146 | — | — | 1 | 7.05 |
| CHEMBL5185902 | — | — | 1 | 7.03 |
| CHEMBL5173332 | — | — | 1 | 6.97 |
| CHEMBL5197306 | — | — | 1 | 6.96 |
| CHEMBL5181013 | — | — | 1 | 6.94 |
| CHEMBL2017974 | BUPARLISIB | 3.0 | 1 | 6.93 |
| CHEMBL2017977 | — | — | 1 | 6.89 |
| CHEMBL5201844 | — | — | 1 | 6.89 |
| CHEMBL5199826 | — | — | 1 | 6.87 |
| CHEMBL5181180 | — | — | 1 | 6.80 |
| CHEMBL5187418 | — | — | 1 | 6.67 |
| CHEMBL5175657 | — | — | 1 | 6.67 |
| CHEMBL5183913 | — | — | 1 | 6.60 |
| CHEMBL5187488 | — | — | 1 | 6.59 |
| CHEMBL5188186 | — | — | 1 | 6.59 |
| CHEMBL5177612 | — | — | 1 | 6.59 |
| CHEMBL5200137 | — | — | 1 | 6.58 |
| CHEMBL5202872 | — | — | 1 | 6.56 |
| CHEMBL5208098 | — | — | 1 | 6.43 |
| CHEMBL5207057 | — | — | 1 | 6.42 |
| CHEMBL5185811 | — | — | 1 | 6.32 |
| CHEMBL5205857 | — | — | 1 | 6.32 |
| CHEMBL5204344 | — | — | 1 | 6.25 |
| CHEMBL5189026 | — | — | 1 | 6.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1879463 | DACTOLISIB | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL5174001 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5203121 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5177354 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL521851 | PICTILISIB | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL2017976 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL5188146 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL5185902 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL5173332 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL5197306 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL5181013 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL2017974 | BUPARLISIB | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL2017977 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5201844 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5199826 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL5181180 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL5187418 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL5175657 | — | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL5183913 | — | IC50 | = | 249.0 | nM | 6.60 |
| CHEMBL5188186 | — | IC50 | = | 256.0 | nM | 6.59 |
| CHEMBL5177612 | — | IC50 | = | 256.0 | nM | 6.59 |
| CHEMBL5187488 | — | IC50 | = | 258.0 | nM | 6.59 |
| CHEMBL5200137 | — | IC50 | = | 264.0 | nM | 6.58 |
| CHEMBL5202872 | — | IC50 | = | 277.0 | nM | 6.56 |
| CHEMBL5208098 | — | IC50 | = | 369.0 | nM | 6.43 |
| CHEMBL5207057 | — | IC50 | = | 376.0 | nM | 6.42 |
| CHEMBL5185811 | — | IC50 | = | 484.0 | nM | 6.32 |
| CHEMBL5205857 | — | IC50 | = | 476.0 | nM | 6.32 |
| CHEMBL5204344 | — | IC50 | = | 558.0 | nM | 6.25 |
| CHEMBL5189026 | — | IC50 | = | 601.0 | nM | 6.22 |
| CHEMBL5192317 | — | IC50 | = | 606.0 | nM | 6.22 |
| CHEMBL5192813 | — | IC50 | = | 739.0 | nM | 6.13 |
| CHEMBL5170832 | — | IC50 | = | 1247.0 | nM | 5.90 |
| CHEMBL5173182 | — | IC50 | = | 1770.0 | nM | 5.75 |
| CHEMBL5170887 | — | IC50 | = | 3060.0 | nM | 5.51 |
| CHEMBL5175263 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL5177019 | — | IC50 | = | 6185.0 | nM | 5.21 |