Assay Detail
Binding
CHEMBL4005474
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Inhibition of human full length PI3K p110delta/p85 alpha using PIP2/ATP as substrate after 30 mins by TR-FRET assay
31
Total Activities
31
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 a Phosphoinositide 3-Kinase (PI3K) β/δ Inhibitor for the Treatment of Phosphatase and Tensin Homolog (PTEN) Deficient Tumors: Building PI3Kβ Potency in a PI3Kδ-Selective Template by Targeting Nonconserved Asp856.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 8.23 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4071605 | — | — | 1 | 9.70 |
| CHEMBL4100135 | — | — | 1 | 9.52 |
| CHEMBL3805137 | — | — | 1 | 9.47 |
| CHEMBL4081433 | — | — | 1 | 9.22 |
| CHEMBL4082130 | — | — | 1 | 9.22 |
| CHEMBL4084645 | — | — | 1 | 9.22 |
| CHEMBL4068742 | — | — | 1 | 9.10 |
| CHEMBL4059461 | — | — | 1 | 8.72 |
| CHEMBL4074361 | — | — | 1 | 8.68 |
| CHEMBL4088324 | — | — | 1 | 8.52 |
| CHEMBL4092381 | — | — | 1 | 8.49 |
| CHEMBL4085918 | — | — | 1 | 8.48 |
| CHEMBL4101102 | — | — | 1 | 8.28 |
| CHEMBL4082978 | — | — | 1 | 8.28 |
| CHEMBL4096052 | — | — | 1 | 8.23 |
| CHEMBL4064384 | — | — | 1 | 8.21 |
| CHEMBL4102306 | — | — | 1 | 8.14 |
| CHEMBL4100094 | — | — | 1 | 8.02 |
| CHEMBL4080464 | — | — | 1 | 8.01 |
| CHEMBL4060084 | — | — | 1 | 7.92 |
| CHEMBL4079545 | — | — | 1 | 7.89 |
| CHEMBL4078045 | — | — | 1 | 7.89 |
| CHEMBL4061937 | — | — | 1 | 7.85 |
| CHEMBL4061095 | — | — | 1 | 7.82 |
| CHEMBL2216870 | IDELALISIB | 4.0 | 1 | 7.75 |
| CHEMBL4098482 | — | — | 1 | 7.68 |
| CHEMBL4086842 | — | — | 1 | 7.58 |
| CHEMBL4067103 | — | — | 1 | 7.29 |
| CHEMBL4080954 | — | — | 1 | 6.88 |
| CHEMBL4103805 | — | — | 1 | 6.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4071605 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4100135 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3805137 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL4081433 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4082130 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4084645 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4068742 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4059461 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4074361 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4088324 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4092381 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4085918 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4101102 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL4082978 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4096052 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL4064384 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL4102306 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4100094 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL4080464 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL4060084 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4079545 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4078045 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4061937 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4061095 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2216870 | IDELALISIB | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4098482 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4086842 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4067103 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4080954 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL4103805 | — | IC50 | = | 309.0 | nM | 6.51 |
| CHEMBL4062975 | — | IC50 | = | 317.0 | nM | 6.50 |