Assay Detail
ADMET
CHEMBL4053404
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins in presence of ATP by HTRF method
19
Total Activities
19
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 alpha isoform (CHEMBL4005) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and Elaboration of a Tractable Tricyclic Scaffold To Synthesize Druglike Inhibitors of Dipeptidyl Peptidase-4 (DPP-4), Antagonists of the C-C Chemokine Receptor Type 5 (CCR5), and Highly Potent and Selective Phosphoinositol-3 Kinase δ (PI3Kδ) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.44 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4071462 | — | — | 1 | 7.50 |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 7.30 |
| CHEMBL4096987 | — | — | 1 | 7.20 |
| CHEMBL4081413 | — | — | 1 | 7.20 |
| CHEMBL4094734 | — | — | 1 | 7.00 |
| CHEMBL4068098 | — | — | 1 | 7.00 |
| CHEMBL4092258 | — | — | 1 | 6.80 |
| CHEMBL4070417 | — | — | 1 | 6.80 |
| CHEMBL4078972 | — | — | 1 | 6.50 |
| CHEMBL4089288 | — | — | 1 | 6.50 |
| CHEMBL4086820 | — | — | 1 | 6.50 |
| CHEMBL4097593 | — | — | 1 | 6.30 |
| CHEMBL2152768 | — | — | 1 | 5.90 |
| CHEMBL4100380 | — | — | 1 | 5.80 |
| CHEMBL4068538 | — | — | 1 | 5.80 |
| CHEMBL4105669 | — | — | 1 | 5.70 |
| CHEMBL4061794 | — | — | 1 | 5.70 |
| CHEMBL4081998 | — | — | 1 | 5.50 |
| CHEMBL4104716 | — | — | 1 | 5.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4071462 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL521851 | PICTILISIB | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL4096987 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4081413 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4094734 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4068098 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4092258 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4070417 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4078972 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL4089288 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL4086820 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL4097593 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL2152768 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL4100380 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4068538 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4105669 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL4061794 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL4081998 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL4104716 | — | IC50 | = | 3981.07 | nM | 5.40 |