Assay Detail
Binding
CHEMBL2090266
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3K alpha by continuous TR-FRET assay
25
Total Activities
25
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
Rational Design, Synthesis, and SAR of a Novel Thiazolopyrimidinone Series of Selective PI3K-beta Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 5.72 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2089120 | — | — | 1 | 6.60 |
| CHEMBL2089119 | — | — | 1 | 6.40 |
| CHEMBL2089114 | — | — | 1 | 6.30 |
| CHEMBL2089112 | — | — | 1 | 6.20 |
| CHEMBL2089103 | — | — | 1 | 6.00 |
| CHEMBL2089109 | — | — | 1 | 5.89 |
| CHEMBL2089116 | — | — | 1 | 5.80 |
| CHEMBL2089117 | — | — | 1 | 5.70 |
| CHEMBL2089118 | — | — | 1 | 5.70 |
| CHEMBL2089107 | — | — | 1 | 5.70 |
| CHEMBL2089100 | — | — | 1 | 5.60 |
| CHEMBL2089105 | — | — | 1 | 5.60 |
| CHEMBL2089106 | — | — | 1 | 5.60 |
| CHEMBL2089111 | — | — | 1 | 5.60 |
| CHEMBL2089097 | — | — | 1 | 5.60 |
| CHEMBL2089101 | — | — | 1 | 5.50 |
| CHEMBL2089104 | — | — | 1 | 5.40 |
| CHEMBL2089096 | — | — | 1 | 5.10 |
| CHEMBL2089115 | — | — | 1 | 4.30 |
| CHEMBL2089102 | — | — | 1 | - |
| CHEMBL2089108 | — | — | 1 | - |
| CHEMBL2089110 | — | — | 1 | - |
| CHEMBL2089099 | — | — | 1 | - |
| CHEMBL2089098 | — | — | 1 | - |
| CHEMBL2089113 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2089120 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL2089119 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL2089114 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL2089112 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL2089103 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2089109 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2089116 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL2089117 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2089118 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2089107 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2089100 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2089105 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2089106 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2089111 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2089097 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2089101 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL2089104 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL2089096 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL2089115 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL2089102 | — | IC50 | > | 3200.0 | nM | - |
| CHEMBL2089108 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL2089110 | — | IC50 | > | 3200.0 | nM | - |
| CHEMBL2089099 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL2089098 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL2089113 | — | IC50 | > | 2500.0 | nM | - |