Assay Detail
Binding
CHEMBL3136755
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PI3Kalpha
22
Total Activities
22
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
Design and synthesis of a novel series of N,4-diphenylpyrimidin-2-amine derivatives as potent and selective PI3K inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.18 | 6.78 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL244559 | — | — | 1 | 6.78 |
| CHEMBL3134612 | — | — | 1 | 6.47 |
| CHEMBL3134620 | — | — | 1 | 6.30 |
| CHEMBL3134607 | — | — | 1 | 6.28 |
| CHEMBL3134606 | — | — | 1 | 6.26 |
| CHEMBL3134618 | — | — | 1 | 6.23 |
| CHEMBL3134605 | — | — | 1 | 6.21 |
| CHEMBL3134619 | — | — | 1 | 6.20 |
| CHEMBL3134611 | — | — | 1 | 6.17 |
| CHEMBL3134608 | — | — | 1 | 6.13 |
| CHEMBL3134604 | — | — | 1 | 6.11 |
| CHEMBL3134615 | — | — | 1 | 6.10 |
| CHEMBL3134601 | — | — | 1 | 6.09 |
| CHEMBL3134621 | — | — | 1 | 6.08 |
| CHEMBL3134602 | — | — | 1 | 6.07 |
| CHEMBL3134610 | — | — | 1 | 6.06 |
| CHEMBL3134613 | — | — | 1 | 6.05 |
| CHEMBL3134616 | — | — | 1 | 6.04 |
| CHEMBL3134603 | — | — | 1 | 6.02 |
| CHEMBL3134617 | — | — | 1 | 6.02 |
| CHEMBL3134609 | — | — | 1 | - |
| CHEMBL3134614 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL244559 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL3134612 | — | IC50 | = | 341.0 | nM | 6.47 |
| CHEMBL3134620 | — | IC50 | = | 503.0 | nM | 6.30 |
| CHEMBL3134607 | — | IC50 | = | 527.0 | nM | 6.28 |
| CHEMBL3134606 | — | IC50 | = | 552.0 | nM | 6.26 |
| CHEMBL3134618 | — | IC50 | = | 591.0 | nM | 6.23 |
| CHEMBL3134605 | — | IC50 | = | 615.0 | nM | 6.21 |
| CHEMBL3134619 | — | IC50 | = | 625.0 | nM | 6.20 |
| CHEMBL3134611 | — | IC50 | = | 679.0 | nM | 6.17 |
| CHEMBL3134608 | — | IC50 | = | 738.0 | nM | 6.13 |
| CHEMBL3134604 | — | IC50 | = | 772.0 | nM | 6.11 |
| CHEMBL3134615 | — | IC50 | = | 792.0 | nM | 6.10 |
| CHEMBL3134601 | — | IC50 | = | 813.0 | nM | 6.09 |
| CHEMBL3134621 | — | IC50 | = | 836.0 | nM | 6.08 |
| CHEMBL3134602 | — | IC50 | = | 851.0 | nM | 6.07 |
| CHEMBL3134610 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL3134613 | — | IC50 | = | 894.0 | nM | 6.05 |
| CHEMBL3134616 | — | IC50 | = | 914.0 | nM | 6.04 |
| CHEMBL3134603 | — | IC50 | = | 953.0 | nM | 6.02 |
| CHEMBL3134617 | — | IC50 | = | 946.0 | nM | 6.02 |
| CHEMBL3134609 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3134614 | — | IC50 | > | 1000.0 | nM | - |