Assay Detail
ADMET
CHEMBL4352637
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Inhibition of N-terminal His6-tagged recombinant full length human p110beta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence polarization assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery, Optimization, and Evaluation of Potent and Highly Selective PI3Kγ-PI3Kδ Dual Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.88 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3039502 | DUVELISIB | 4.0 | 1 | 8.10 |
| CHEMBL4471912 | — | — | 1 | 7.60 |
| CHEMBL4514752 | — | — | 1 | 7.47 |
| CHEMBL4446047 | — | — | 1 | 7.29 |
| CHEMBL4438693 | — | — | 1 | 7.04 |
| CHEMBL4463472 | — | — | 1 | 6.78 |
| CHEMBL4520300 | — | — | 1 | 6.77 |
| CHEMBL4522342 | — | — | 1 | 6.72 |
| CHEMBL2216870 | IDELALISIB | 4.0 | 1 | 6.53 |
| CHEMBL4549473 | — | — | 1 | 6.53 |
| CHEMBL4548876 | — | — | 1 | 6.38 |
| CHEMBL4513442 | — | — | 1 | 6.23 |
| CHEMBL4445566 | — | — | 1 | 6.03 |
| CHEMBL4469444 | — | — | 1 | - |
| CHEMBL4459544 | — | — | 1 | - |
| CHEMBL4541260 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3039502 | DUVELISIB | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4471912 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4514752 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4446047 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4438693 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL4463472 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL4520300 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4522342 | — | IC50 | = | 191.0 | nM | 6.72 |
| CHEMBL2216870 | IDELALISIB | IC50 | = | 293.0 | nM | 6.53 |
| CHEMBL4549473 | — | IC50 | = | 298.0 | nM | 6.53 |
| CHEMBL4548876 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4513442 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL4445566 | — | IC50 | = | 945.0 | nM | 6.03 |
| CHEMBL4469444 | — | IC50 | - | — | - | |
| CHEMBL4459544 | — | IC50 | - | — | - | |
| CHEMBL4541260 | — | IC50 | > | 1000.0 | nM | - |