Assay Detail
Binding
CHEMBL887586
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Inhibition of p110alpha by SPA assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (CHEMBL4005) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological evaluation of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.92 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL541643 | — | — | 1 | 8.60 |
| CHEMBL538346 | — | — | 1 | 8.44 |
| CHEMBL3216006 | — | — | 1 | 7.80 |
| CHEMBL534951 | — | — | 1 | 7.62 |
| CHEMBL541906 | — | — | 1 | 7.58 |
| CHEMBL3215760 | — | — | 1 | 7.10 |
| CHEMBL537877 | — | — | 1 | 7.00 |
| CHEMBL3216649 | — | — | 1 | 6.85 |
| CHEMBL388480 | — | — | 1 | 6.80 |
| CHEMBL3216005 | — | — | 1 | 6.77 |
| CHEMBL390623 | — | — | 1 | 6.40 |
| CHEMBL230131 | — | — | 1 | 6.25 |
| CHEMBL98350 | LY-294002 | -1.0 | 1 | 6.20 |
| CHEMBL390850 | — | — | 1 | 5.85 |
| CHEMBL230239 | — | — | 1 | 5.77 |
| CHEMBL541647 | — | — | 1 | 5.62 |
| CHEMBL230778 | — | — | 1 | - |
| CHEMBL390852 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL541643 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL538346 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL3216006 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL534951 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL541906 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3215760 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL537877 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3216649 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL388480 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3216005 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL390623 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL230131 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL98350 | LY-294002 | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL390850 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL230239 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL541647 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL230778 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL390852 | — | IC50 | > | 30000.0 | nM | - |