Assay Detail
ADMET
CHEMBL4134209
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Inhibition of recombinant PI3Kbeta (unknown origin) using phosphatidyl inositol/n-Octyl-glucoside as substrate measured after 60 mins by KinaseGlo assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (CHEMBL3145) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.78 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3643414 | — | — | 1 | 6.52 |
| CHEMBL3643413 | LENIOLISIB | 4.0 | 1 | 6.37 |
| CHEMBL3643427 | — | — | 1 | 6.02 |
| CHEMBL3643407 | — | — | 1 | 5.88 |
| CHEMBL3977066 | — | — | 1 | 5.78 |
| CHEMBL3643409 | — | — | 1 | 5.77 |
| CHEMBL3643429 | — | — | 1 | 5.70 |
| CHEMBL3643349 | — | — | 1 | 5.38 |
| CHEMBL3947814 | — | — | 1 | 5.32 |
| CHEMBL4171158 | — | — | 1 | 5.05 |
| CHEMBL4164149 | — | — | 1 | - |
| CHEMBL4163245 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3643414 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3643413 | LENIOLISIB | IC50 | = | 424.0 | nM | 6.37 |
| CHEMBL3643427 | — | IC50 | = | 951.0 | nM | 6.02 |
| CHEMBL3643407 | — | IC50 | = | 1330.0 | nM | 5.88 |
| CHEMBL3977066 | — | IC50 | = | 1650.0 | nM | 5.78 |
| CHEMBL3643409 | — | IC50 | = | 1710.0 | nM | 5.77 |
| CHEMBL3643429 | — | IC50 | = | 2020.0 | nM | 5.70 |
| CHEMBL3643349 | — | IC50 | = | 4150.0 | nM | 5.38 |
| CHEMBL3947814 | — | IC50 | = | 4840.0 | nM | 5.32 |
| CHEMBL4171158 | — | IC50 | = | 8940.0 | nM | 5.05 |
| CHEMBL4164149 | — | IC50 | > | 9100.0 | nM | - |
| CHEMBL4163245 | — | IC50 | > | 9100.0 | nM | - |