Assay Detail
Binding
CHEMBL4619038
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Inhibition of human p110delta catalytic subunit/p85alpha 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 |
| 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 | 6.66 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4646376 | — | — | 1 | 7.92 |
| CHEMBL4639049 | — | — | 1 | 7.46 |
| CHEMBL3408248 | AZD-8186 | 1.0 | 1 | 7.44 |
| CHEMBL4470860 | — | — | 3 | 7.38 |
| CHEMBL4643981 | — | — | 1 | 7.28 |
| CHEMBL4639252 | — | — | 3 | 7.08 |
| CHEMBL4634912 | — | — | 1 | 7.00 |
| CHEMBL4647791 | — | — | 3 | 7.00 |
| CHEMBL4637136 | — | — | 3 | 6.91 |
| CHEMBL4634167 | — | — | 3 | 6.90 |
| CHEMBL4641819 | — | — | 1 | 6.53 |
| CHEMBL4648699 | — | — | 1 | 6.52 |
| CHEMBL3188551 | GSK-2636771 | 2.0 | 1 | 6.52 |
| CHEMBL4632733 | — | — | 1 | 6.40 |
| CHEMBL1972466 | — | — | 1 | 6.30 |
| CHEMBL4639367 | — | — | 1 | 5.94 |
| CHEMBL4634032 | — | — | 1 | 5.78 |
| CHEMBL4647885 | — | — | 1 | 5.59 |
| CHEMBL4643832 | — | — | 1 | - |
| CHEMBL4636419 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4646376 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4639049 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3408248 | AZD-8186 | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4470860 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4470860 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4643981 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4639252 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4647791 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL4634912 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4639252 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL4637136 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL4634167 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL4647791 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4634167 | — | IC50 | = | 222.0 | nM | 6.65 |
| CHEMBL4641819 | — | IC50 | = | 297.0 | nM | 6.53 |
| CHEMBL4648699 | — | IC50 | = | 302.0 | nM | 6.52 |
| CHEMBL3188551 | GSK-2636771 | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4637136 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4632733 | — | IC50 | = | 402.0 | nM | 6.40 |
| CHEMBL1972466 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4637136 | — | IC50 | = | 1108.0 | nM | 5.96 |
| CHEMBL4639367 | — | IC50 | = | 1144.0 | nM | 5.94 |
| CHEMBL4639252 | — | IC50 | = | 1464.0 | nM | 5.83 |
| CHEMBL4634032 | — | IC50 | = | 1657.0 | nM | 5.78 |
| CHEMBL4647885 | — | IC50 | = | 2586.0 | nM | 5.59 |
| CHEMBL4634167 | — | IC50 | = | 4837.0 | nM | 5.32 |
| CHEMBL4470860 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4647791 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4643832 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4636419 | — | IC50 | > | 10000.0 | nM | - |