Assay Detail
Binding
CHEMBL3610609
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kalpha (unknown origin) using phosphatidylinositol as substrate preincubated for 15 mins followed by ATP addition measured after 1 hr by KinaseGlo luminescence assay
18
Total Activities
18
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 |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (CHEMBL4005) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 8.06 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3609522 | — | — | 1 | 8.40 |
| CHEMBL3609529 | — | — | 1 | 8.40 |
| CHEMBL3609527 | — | — | 1 | 8.30 |
| CHEMBL3609526 | — | — | 1 | 8.30 |
| CHEMBL3609523 | — | — | 1 | 8.30 |
| CHEMBL3609525 | — | — | 1 | 8.22 |
| CHEMBL3609524 | — | — | 1 | 8.22 |
| CHEMBL2397186 | — | — | 1 | 8.15 |
| CHEMBL3609516 | — | — | 1 | 8.10 |
| CHEMBL3609520 | — | — | 1 | 8.05 |
| CHEMBL3609517 | — | — | 1 | 8.05 |
| CHEMBL3609521 | — | — | 1 | 8.00 |
| CHEMBL3609519 | — | — | 1 | 7.96 |
| CHEMBL3609514 | — | — | 1 | 7.89 |
| CHEMBL3609518 | — | — | 1 | 7.89 |
| CHEMBL3609528 | — | — | 1 | 7.85 |
| CHEMBL3218581 | — | — | 1 | 7.82 |
| CHEMBL3609515 | — | — | 1 | 7.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3609522 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3609529 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3609527 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3609526 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3609523 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3609525 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3609524 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL2397186 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3609516 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3609520 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3609517 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3609521 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3609519 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3609514 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3609518 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3609528 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3218581 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3609515 | — | IC50 | = | 70.0 | nM | 7.16 |