Assay Detail
Binding
CHEMBL3366862
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kbeta in human MAD-MB-468 cells assessed as inhibition of Ser473 Akt phosphorylation by cellular potency assay
28
Total Activities
28
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 beta isoform (CHEMBL3145) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 9-(1-anilinoethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.62 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3319646 | — | — | 1 | 8.70 |
| CHEMBL3319490 | — | — | 1 | 8.52 |
| CHEMBL3319485 | — | — | 1 | 8.40 |
| CHEMBL3319644 | — | — | 1 | 8.15 |
| CHEMBL3319494 | — | — | 1 | 8.10 |
| CHEMBL3318715 | — | — | 1 | 8.10 |
| CHEMBL3319642 | — | — | 1 | 8.05 |
| CHEMBL3319643 | — | — | 1 | 8.00 |
| CHEMBL3319492 | — | — | 1 | 7.96 |
| CHEMBL3319491 | — | — | 1 | 7.96 |
| CHEMBL3319645 | — | — | 1 | 7.92 |
| CHEMBL3319641 | — | — | 1 | 7.77 |
| CHEMBL1972466 | — | — | 1 | 7.66 |
| CHEMBL3319647 | — | — | 1 | 7.64 |
| CHEMBL3319493 | — | — | 1 | 7.60 |
| CHEMBL3319495 | — | — | 1 | 7.60 |
| CHEMBL3319496 | — | — | 1 | 7.54 |
| CHEMBL3319489 | — | — | 1 | 7.47 |
| CHEMBL3319487 | — | — | 1 | 7.41 |
| CHEMBL2165191 | AZD-6482 | 2.0 | 1 | 7.40 |
| CHEMBL3319486 | — | — | 1 | 7.21 |
| CHEMBL3319488 | — | — | 1 | 7.14 |
| CHEMBL3319648 | — | — | 1 | 7.13 |
| CHEMBL3317473 | — | — | 1 | 7.12 |
| CHEMBL3319639 | — | — | 1 | 7.09 |
| CHEMBL3318711 | — | — | 1 | 6.81 |
| CHEMBL3319640 | — | — | 1 | 6.72 |
| CHEMBL3319649 | — | — | 1 | 6.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3319646 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3319490 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3319485 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3319644 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3319494 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3318715 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3319642 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3319643 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3319492 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3319491 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3319645 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3319641 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1972466 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3319647 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3319493 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3319495 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3319496 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3319489 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3319487 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL2165191 | AZD-6482 | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3319486 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL3319488 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL3319648 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL3317473 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL3319639 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL3318711 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL3319640 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3319649 | — | IC50 | = | 530.0 | nM | 6.28 |