Assay Detail
ADMET
CHEMBL4005472
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Inhibition of human full length PI3K p110alpha/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 | ADMET |
| 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 | 6.27 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4071605 | — | — | 1 | 7.64 |
| CHEMBL4068742 | — | — | 1 | 7.35 |
| CHEMBL4082130 | — | — | 1 | 7.09 |
| CHEMBL4081433 | — | — | 1 | 7.08 |
| CHEMBL4084645 | — | — | 1 | 7.05 |
| CHEMBL4064384 | — | — | 1 | 6.77 |
| CHEMBL4100094 | — | — | 1 | 6.73 |
| CHEMBL4100135 | — | — | 1 | 6.55 |
| CHEMBL4085918 | — | — | 1 | 6.55 |
| CHEMBL4088324 | — | — | 1 | 6.54 |
| CHEMBL4074361 | — | — | 1 | 6.52 |
| CHEMBL4096052 | — | — | 1 | 6.51 |
| CHEMBL4080464 | — | — | 1 | 6.49 |
| CHEMBL4060084 | — | — | 1 | 6.45 |
| CHEMBL4079545 | — | — | 1 | 6.16 |
| CHEMBL4086842 | — | — | 1 | 6.14 |
| CHEMBL4102306 | — | — | 1 | 6.12 |
| CHEMBL4082978 | — | — | 1 | 6.07 |
| CHEMBL4101102 | — | — | 1 | 5.97 |
| CHEMBL4098482 | — | — | 1 | 5.96 |
| CHEMBL4078045 | — | — | 1 | 5.88 |
| CHEMBL4067103 | — | — | 1 | 5.82 |
| CHEMBL4061937 | — | — | 1 | 5.80 |
| CHEMBL3805137 | — | — | 1 | 5.69 |
| CHEMBL4061095 | — | — | 1 | 5.68 |
| CHEMBL4092381 | — | — | 1 | 5.46 |
| CHEMBL4059461 | — | — | 1 | 5.45 |
| CHEMBL4080954 | — | — | 1 | 5.16 |
| CHEMBL2216870 | IDELALISIB | 4.0 | 1 | 5.12 |
| CHEMBL4103805 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4071605 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4068742 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4082130 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4081433 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4084645 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4064384 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL4100094 | — | IC50 | = | 187.0 | nM | 6.73 |
| CHEMBL4100135 | — | IC50 | = | 281.0 | nM | 6.55 |
| CHEMBL4085918 | — | IC50 | = | 284.0 | nM | 6.55 |
| CHEMBL4088324 | — | IC50 | = | 291.0 | nM | 6.54 |
| CHEMBL4074361 | — | IC50 | = | 302.0 | nM | 6.52 |
| CHEMBL4096052 | — | IC50 | = | 308.0 | nM | 6.51 |
| CHEMBL4080464 | — | IC50 | = | 322.0 | nM | 6.49 |
| CHEMBL4060084 | — | IC50 | = | 357.0 | nM | 6.45 |
| CHEMBL4079545 | — | IC50 | = | 686.0 | nM | 6.16 |
| CHEMBL4086842 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL4102306 | — | IC50 | = | 756.0 | nM | 6.12 |
| CHEMBL4082978 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL4101102 | — | IC50 | = | 1074.0 | nM | 5.97 |
| CHEMBL4098482 | — | IC50 | = | 1085.0 | nM | 5.96 |
| CHEMBL4078045 | — | IC50 | = | 1303.0 | nM | 5.88 |
| CHEMBL4067103 | — | IC50 | = | 1511.0 | nM | 5.82 |
| CHEMBL4061937 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3805137 | — | IC50 | = | 2025.0 | nM | 5.69 |
| CHEMBL4061095 | — | IC50 | = | 2080.0 | nM | 5.68 |
| CHEMBL4092381 | — | IC50 | = | 3490.0 | nM | 5.46 |
| CHEMBL4059461 | — | IC50 | = | 3538.0 | nM | 5.45 |
| CHEMBL4080954 | — | IC50 | = | 6937.0 | nM | 5.16 |
| CHEMBL2216870 | IDELALISIB | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL4103805 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4062975 | — | IC50 | > | 10000.0 | nM | - |