Assay Detail
Binding
CHEMBL4352645
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Inhibition of PI3Kgamma in rat RAW264.7 cells assessed as reduction in C5a-stimulated AKT phosphorylation at Ser473 residue preincubated for 30 mins followed by C5a-stimulation and measured after 5 mins
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | RAW264.7 |
| Confidence | 0 — Uncurated / Unknown |
| 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 | 19 | 7.34 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4522342 | — | — | 1 | 8.15 |
| CHEMBL4574883 | — | — | 1 | 8.10 |
| CHEMBL4548876 | — | — | 1 | 7.70 |
| CHEMBL4549473 | — | — | 1 | 7.66 |
| CHEMBL3039502 | DUVELISIB | 4.0 | 1 | 7.60 |
| CHEMBL4530831 | — | — | 1 | 7.40 |
| CHEMBL4463472 | — | — | 1 | 7.38 |
| CHEMBL4468887 | — | — | 1 | 6.85 |
| CHEMBL4445566 | — | — | 1 | 6.82 |
| CHEMBL4467526 | — | — | 1 | 6.62 |
| CHEMBL2216870 | IDELALISIB | 4.0 | 1 | 6.47 |
| CHEMBL4446047 | — | — | 1 | - |
| CHEMBL4520300 | — | — | 1 | - |
| CHEMBL4471912 | — | — | 1 | - |
| CHEMBL4443601 | — | — | 1 | - |
| CHEMBL4446644 | — | — | 1 | - |
| CHEMBL4442420 | — | — | 1 | - |
| CHEMBL4514752 | — | — | 1 | - |
| CHEMBL4438693 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4522342 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4574883 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4548876 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4549473 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3039502 | DUVELISIB | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4530831 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4463472 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4468887 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL4445566 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL4467526 | — | IC50 | = | 241.0 | nM | 6.62 |
| CHEMBL2216870 | IDELALISIB | IC50 | = | 337.0 | nM | 6.47 |
| CHEMBL4446047 | — | IC50 | - | — | - | |
| CHEMBL4520300 | — | IC50 | - | — | - | |
| CHEMBL4471912 | — | IC50 | - | — | - | |
| CHEMBL4443601 | — | IC50 | - | — | - | |
| CHEMBL4446644 | — | IC50 | - | — | - | |
| CHEMBL4442420 | — | IC50 | - | — | - | |
| CHEMBL4514752 | — | IC50 | - | — | - | |
| CHEMBL4438693 | — | IC50 | - | — | - |