Assay Detail
Binding
CHEMBL4836858
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Inhibition of recombinant human full length N-terminal His-tagged p110alpha/p85alpha expressed in baculovirus expression system measured after 60 mins in presence of ATP by ATP-competitive binding assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of novel purinyl quinazolinone derivatives as PI3Kδ-specific inhibitors for the treatment of hematologic malignancies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.49 | 6.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4871071 | — | — | 1 | 6.90 |
| CHEMBL4868117 | — | — | 1 | 6.87 |
| CHEMBL4845946 | — | — | 1 | 6.82 |
| CHEMBL4862467 | — | — | 1 | 6.69 |
| CHEMBL4852166 | — | — | 1 | 6.65 |
| CHEMBL4874404 | — | — | 1 | 6.53 |
| CHEMBL4876309 | — | — | 1 | 6.52 |
| CHEMBL4854194 | — | — | 1 | 6.49 |
| CHEMBL4853740 | — | — | 1 | 6.45 |
| CHEMBL4858100 | — | — | 1 | 6.43 |
| CHEMBL4874496 | — | — | 1 | 6.42 |
| CHEMBL2216870 | IDELALISIB | 4.0 | 1 | 6.39 |
| CHEMBL4852863 | — | — | 1 | 6.32 |
| CHEMBL4876188 | — | — | 1 | 6.31 |
| CHEMBL4847494 | — | — | 1 | 6.06 |
| CHEMBL4870032 | — | — | 1 | 6.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4871071 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL4868117 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL4845946 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL4862467 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL4852166 | — | IC50 | = | 222.0 | nM | 6.65 |
| CHEMBL4874404 | — | IC50 | = | 295.0 | nM | 6.53 |
| CHEMBL4876309 | — | IC50 | = | 301.0 | nM | 6.52 |
| CHEMBL4854194 | — | IC50 | = | 326.0 | nM | 6.49 |
| CHEMBL4853740 | — | IC50 | = | 356.0 | nM | 6.45 |
| CHEMBL4858100 | — | IC50 | = | 369.0 | nM | 6.43 |
| CHEMBL4874496 | — | IC50 | = | 385.0 | nM | 6.42 |
| CHEMBL2216870 | IDELALISIB | IC50 | = | 409.0 | nM | 6.39 |
| CHEMBL4852863 | — | IC50 | = | 475.0 | nM | 6.32 |
| CHEMBL4876188 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4847494 | — | IC50 | = | 878.0 | nM | 6.06 |
| CHEMBL4870032 | — | IC50 | = | 879.0 | nM | 6.06 |