Assay Detail
Binding
CHEMBL2020200
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Inhibition of PI3Kalpha
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous 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
Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 8.11 | 9.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2017653 | — | — | 1 | 9.46 |
| CHEMBL1234354 | PF-04691502 | 2.0 | 1 | 9.24 |
| CHEMBL2017654 | — | — | 1 | 9.22 |
| CHEMBL2017648 | — | — | 1 | 8.77 |
| CHEMBL2017649 | — | — | 1 | 8.74 |
| CHEMBL2017650 | — | — | 1 | 8.52 |
| CHEMBL2017647 | — | — | 1 | 7.89 |
| CHEMBL2017651 | — | — | 1 | 6.76 |
| CHEMBL570592 | — | — | 1 | 6.64 |
| CHEMBL2017652 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2017653 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL1234354 | PF-04691502 | Ki | = | 0.57 | nM | 9.24 |
| CHEMBL2017654 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL2017648 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL2017649 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL2017650 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL2017647 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL2017651 | — | Ki | = | 175.0 | nM | 6.76 |
| CHEMBL570592 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL2017652 | — | Ki | = | 1280.0 | nM | 5.89 |