Assay Detail
Binding
CHEMBL4134211
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Inhibition of PI3Kdelta (unknown origin) using phosphatidyl inositol as substrate measured after 60 mins by Alexa Fluor647-labelled ADP tracer based TR-FRET assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (CHEMBL3130) ↗| 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 | 7.55 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3643414 | — | — | 1 | 8.40 |
| CHEMBL3977066 | — | — | 1 | 8.05 |
| CHEMBL3643413 | LENIOLISIB | 4.0 | 1 | 7.96 |
| CHEMBL3643427 | — | — | 1 | 7.70 |
| CHEMBL3643409 | — | — | 1 | 7.57 |
| CHEMBL3643407 | — | — | 1 | 7.55 |
| CHEMBL3947814 | — | — | 1 | 7.54 |
| CHEMBL3643429 | — | — | 1 | 7.52 |
| CHEMBL4164149 | — | — | 1 | 7.19 |
| CHEMBL3643349 | — | — | 1 | 7.12 |
| CHEMBL4163245 | — | — | 1 | 7.08 |
| CHEMBL4171158 | — | — | 1 | 6.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3643414 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3977066 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3643413 | LENIOLISIB | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3643427 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3643409 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3643407 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3947814 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3643429 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4164149 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3643349 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4163245 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4171158 | — | IC50 | = | 132.0 | nM | 6.88 |