Assay Detail
Binding
CHEMBL4619036
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human full-length N-terminal His6-tagged p110beta/human recombinant full-length untagged p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate after 30 mins in presence of ATP at 2xKm concentration by TR-FRET assay
30
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of an Atropisomeric PI3Kβ Selective Inhibitor through Optimization of the Hinge Binding Motif.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.50 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4470860 | — | — | 3 | 8.70 |
| CHEMBL4647791 | — | — | 3 | 8.70 |
| CHEMBL3408248 | AZD-8186 | 1.0 | 1 | 8.52 |
| CHEMBL4646376 | — | — | 1 | 8.52 |
| CHEMBL4634912 | — | — | 1 | 8.30 |
| CHEMBL4634167 | — | — | 3 | 8.22 |
| CHEMBL4643981 | — | — | 1 | 8.15 |
| CHEMBL4637136 | — | — | 3 | 8.05 |
| CHEMBL4639252 | — | — | 3 | 8.05 |
| CHEMBL4639049 | — | — | 1 | 7.92 |
| CHEMBL4641819 | — | — | 1 | 7.72 |
| CHEMBL3188551 | GSK-2636771 | 2.0 | 1 | 7.60 |
| CHEMBL4632733 | — | — | 1 | 7.52 |
| CHEMBL4648699 | — | — | 1 | 7.30 |
| CHEMBL4639367 | — | — | 1 | 7.21 |
| CHEMBL1972466 | — | — | 1 | 7.20 |
| CHEMBL4634032 | — | — | 1 | 6.49 |
| CHEMBL4647885 | — | — | 1 | 6.47 |
| CHEMBL4636419 | — | — | 1 | 5.85 |
| CHEMBL4643832 | — | — | 1 | 5.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4647791 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4470860 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3408248 | AZD-8186 | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4646376 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4470860 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4647791 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4634912 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4634167 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4643981 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4634167 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4639252 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4637136 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4637136 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4639252 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4639049 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4641819 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3188551 | GSK-2636771 | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4632733 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4648699 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4639367 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL1972466 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4637136 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4639252 | — | IC50 | = | 206.0 | nM | 6.69 |
| CHEMBL4634032 | — | IC50 | = | 321.0 | nM | 6.49 |
| CHEMBL4647885 | — | IC50 | = | 341.0 | nM | 6.47 |
| CHEMBL4634167 | — | IC50 | = | 545.0 | nM | 6.26 |
| CHEMBL4647791 | — | IC50 | = | 562.0 | nM | 6.25 |
| CHEMBL4470860 | — | IC50 | = | 1423.0 | nM | 5.85 |
| CHEMBL4636419 | — | IC50 | = | 1402.0 | nM | 5.85 |
| CHEMBL4643832 | — | IC50 | = | 2857.0 | nM | 5.54 |