Assay Detail
Binding
CHEMBL3592016
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Inhibition of Glu-tagged PI3KC2beta (unknown origin) expressed in Sf9/Baculovirus system using [gamma-33P]ATP by scintillation proximity assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta (CHEMBL5554) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis and biological evaluation of novel condensed pyrrolo[1,2-c]pyrimidines featuring morpholine moiety as PI3Kα inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 4.84 | 5.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3589370 | — | — | 1 | 5.57 |
| CHEMBL3589371 | — | — | 1 | 5.35 |
| CHEMBL3589324 | — | — | 1 | 5.28 |
| CHEMBL3589377 | — | — | 1 | 5.07 |
| CHEMBL3589378 | — | — | 1 | 5.07 |
| CHEMBL3589379 | — | — | 1 | 5.06 |
| CHEMBL3589372 | — | — | 1 | 5.03 |
| CHEMBL3589376 | — | — | 1 | 5.01 |
| CHEMBL3589321 | — | — | 1 | 4.87 |
| CHEMBL3589322 | — | — | 1 | 4.84 |
| CHEMBL3589320 | — | — | 1 | 4.68 |
| CHEMBL3589374 | — | — | 1 | 4.54 |
| CHEMBL3589373 | — | — | 1 | 4.10 |
| CHEMBL3589375 | — | — | 1 | 4.09 |
| CHEMBL3589323 | — | — | 1 | 4.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3589370 | — | IC50 | = | 2670.0 | nM | 5.57 |
| CHEMBL3589371 | — | IC50 | = | 4430.0 | nM | 5.35 |
| CHEMBL3589324 | — | IC50 | = | 5250.0 | nM | 5.28 |
| CHEMBL3589377 | — | IC50 | = | 8460.0 | nM | 5.07 |
| CHEMBL3589378 | — | IC50 | = | 8560.0 | nM | 5.07 |
| CHEMBL3589379 | — | IC50 | = | 8750.0 | nM | 5.06 |
| CHEMBL3589372 | — | IC50 | = | 9450.0 | nM | 5.03 |
| CHEMBL3589376 | — | IC50 | = | 9760.0 | nM | 5.01 |
| CHEMBL3589321 | — | IC50 | = | 13560.0 | nM | 4.87 |
| CHEMBL3589322 | — | IC50 | = | 14560.0 | nM | 4.84 |
| CHEMBL3589320 | — | IC50 | = | 20840.0 | nM | 4.68 |
| CHEMBL3589374 | — | IC50 | = | 28640.0 | nM | 4.54 |
| CHEMBL3589373 | — | IC50 | = | 78780.0 | nM | 4.10 |
| CHEMBL3589375 | — | IC50 | = | 81560.0 | nM | 4.09 |
| CHEMBL3589323 | — | IC50 | = | 85540.0 | nM | 4.07 |