Assay Detail
Binding
CHEMBL4392569
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PI3Kdelta using PIP2 as substrate after 1 hr
22
Total Activities
22
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 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 8.06 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4560054 | — | — | 1 | 8.72 |
| CHEMBL2216870 | IDELALISIB | 4.0 | 1 | 8.68 |
| CHEMBL4550603 | — | — | 1 | 8.39 |
| CHEMBL4535169 | — | — | 1 | 8.23 |
| CHEMBL4440218 | — | — | 1 | 8.21 |
| CHEMBL1879463 | DACTOLISIB | 3.0 | 1 | 8.10 |
| CHEMBL4454741 | — | — | 1 | 8.02 |
| CHEMBL4467333 | — | — | 1 | 7.96 |
| CHEMBL4589873 | — | — | 1 | 7.94 |
| CHEMBL4536349 | — | — | 1 | 7.74 |
| CHEMBL4542493 | — | — | 1 | 7.70 |
| CHEMBL4462149 | — | — | 1 | 7.55 |
| CHEMBL4563971 | — | — | 1 | 7.53 |
| CHEMBL4537987 | — | — | 1 | - |
| CHEMBL4461158 | — | — | 1 | - |
| CHEMBL4558021 | — | — | 1 | - |
| CHEMBL4438163 | — | — | 1 | - |
| CHEMBL4514522 | — | — | 1 | - |
| CHEMBL4450071 | — | — | 1 | - |
| CHEMBL4515364 | — | — | 1 | - |
| CHEMBL4474240 | — | — | 1 | - |
| CHEMBL4564102 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4560054 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL2216870 | IDELALISIB | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4550603 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4535169 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL4440218 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL1879463 | DACTOLISIB | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4454741 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL4467333 | — | IC50 | = | 11.1 | nM | 7.96 |
| CHEMBL4589873 | — | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL4536349 | — | IC50 | = | 18.4 | nM | 7.74 |
| CHEMBL4542493 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4462149 | — | IC50 | = | 28.3 | nM | 7.55 |
| CHEMBL4563971 | — | IC50 | = | 29.4 | nM | 7.53 |
| CHEMBL4537987 | — | IC50 | - | — | - | |
| CHEMBL4461158 | — | IC50 | - | — | - | |
| CHEMBL4558021 | — | IC50 | - | — | - | |
| CHEMBL4438163 | — | IC50 | - | — | - | |
| CHEMBL4514522 | — | IC50 | - | — | - | |
| CHEMBL4450071 | — | IC50 | - | — | - | |
| CHEMBL4515364 | — | IC50 | - | — | - | |
| CHEMBL4474240 | — | IC50 | - | — | - | |
| CHEMBL4564102 | — | IC50 | - | — | - |