Assay Detail
Binding
CHEMBL3887329
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Homogenous Time Resolved Fluorescence (HTRF) Assay: The homogenous time resolved fluorescence (HTRF) assay allows detection of 3,4,5-triphosphate (PIP3) formed as a result of phosphorylation of phosphotidylinositol 4,5-biphosphate (PIP2) by PI3K isoforms such as alpha, beta, gamma or delta PI3K isoform activity for alpha, beta, gamma or delta was determined using a PI3K human HTRF Assay Kit (Millipore, Billerica, Mass.) with modifications. All incubations were carried out at room temperature. Briefly, 0.5 ul of 40x inhibitor (in 100% DMSO) or 100% DMSO were added to each well of a 384-well black plate (Greiner Bio-One, Monroe, N.C.) containing 14.5ul 1x reaction buffer/PIP2 (10 mM MgCl2, 5 mM DTT, 1.38 uM PIP2) mix with or without enzyme and incubated for 10 min. After the initial incubation, 5 ul/well of 400 uM ATP was added and incubated for an additional 30 minutes. Reaction was terminated by adding 5 ul/well stop solution (Millipore, Billerica, Mass.).
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 8 — Homologous 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
Selective PI3K delta inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.28 | 7.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3904566 | — | — | 1 | 7.86 |
| CHEMBL3948730 | UMBRALISIB | 4.0 | 1 | 7.65 |
| CHEMBL3978564 | — | — | 1 | 7.60 |
| CHEMBL3980557 | — | — | 1 | 7.43 |
| CHEMBL4115084 | — | — | 1 | 5.84 |
| CHEMBL4111394 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3904566 | — | IC50 | = | 13.83 | nM | 7.86 |
| CHEMBL3948730 | UMBRALISIB | IC50 | = | 22.33 | nM | 7.65 |
| CHEMBL3978564 | — | IC50 | = | 24.89 | nM | 7.60 |
| CHEMBL3980557 | — | IC50 | = | 37.32 | nM | 7.43 |
| CHEMBL4115084 | — | IC50 | = | 1447.0 | nM | 5.84 |
| CHEMBL4111394 | — | IC50 | > | 10000.0 | nM | - |