Assay Detail
Binding
CHEMBL5155270
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kdelta (unknown origin) using PIP2 as substrate preincubated for 1 hr followed by substrate addition and measured after 60 mins in presence of ATP by ADP-glo assay
49
Total Activities
49
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
Design, Synthesis, and Structure-Activity Relationship Optimization of Pyrazolopyrimidine Amide Inhibitors of Phosphoinositide 3-Kinase γ (PI3Kγ).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 49 | 6.22 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5179088 | — | — | 1 | 7.70 |
| CHEMBL5204993 | — | — | 1 | 7.70 |
| CHEMBL5186057 | — | — | 1 | 7.21 |
| CHEMBL5174699 | — | — | 1 | 7.17 |
| CHEMBL5190157 | — | — | 1 | 7.08 |
| CHEMBL5171703 | — | — | 1 | 7.07 |
| CHEMBL5200068 | — | — | 1 | 6.91 |
| CHEMBL5186453 | — | — | 1 | 6.84 |
| CHEMBL5201323 | — | — | 1 | 6.81 |
| CHEMBL5182329 | — | — | 1 | 6.76 |
| CHEMBL5182177 | — | — | 1 | 6.75 |
| CHEMBL5194953 | — | — | 1 | 6.59 |
| CHEMBL5206549 | — | — | 1 | 6.57 |
| CHEMBL5194457 | — | — | 1 | 6.42 |
| CHEMBL5201929 | — | — | 1 | 6.38 |
| CHEMBL5204743 | — | — | 1 | 6.38 |
| CHEMBL5172752 | — | — | 1 | 6.34 |
| CHEMBL5202602 | — | — | 1 | 6.25 |
| CHEMBL5203565 | — | — | 1 | 6.22 |
| CHEMBL5177379 | — | — | 1 | 6.16 |
| CHEMBL5206156 | — | — | 1 | 6.15 |
| CHEMBL5172570 | — | — | 1 | 6.11 |
| CHEMBL5171652 | — | — | 1 | 6.08 |
| CHEMBL5189490 | — | — | 1 | 6.08 |
| CHEMBL5173627 | — | — | 1 | 6.08 |
| CHEMBL5175755 | — | — | 1 | 6.04 |
| CHEMBL5171421 | — | — | 1 | 6.00 |
| CHEMBL5172719 | — | — | 1 | 5.97 |
| CHEMBL5209268 | — | — | 1 | 5.97 |
| CHEMBL5207086 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5179088 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5204993 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5186057 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL5174699 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL5190157 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL5171703 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL5200068 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL5186453 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL5201323 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL5182329 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL5182177 | — | IC50 | = | 179.0 | nM | 6.75 |
| CHEMBL5194953 | — | IC50 | = | 256.0 | nM | 6.59 |
| CHEMBL5206549 | — | IC50 | = | 268.0 | nM | 6.57 |
| CHEMBL5194457 | — | IC50 | = | 376.0 | nM | 6.42 |
| CHEMBL5204743 | — | IC50 | = | 417.0 | nM | 6.38 |
| CHEMBL5201929 | — | IC50 | = | 419.0 | nM | 6.38 |
| CHEMBL5172752 | — | IC50 | = | 459.0 | nM | 6.34 |
| CHEMBL5202602 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL5203565 | — | IC50 | = | 598.0 | nM | 6.22 |
| CHEMBL5177379 | — | IC50 | = | 698.0 | nM | 6.16 |
| CHEMBL5206156 | — | IC50 | = | 714.0 | nM | 6.15 |
| CHEMBL5172570 | — | IC50 | = | 769.0 | nM | 6.11 |
| CHEMBL5173627 | — | IC50 | = | 835.0 | nM | 6.08 |
| CHEMBL5171652 | — | IC50 | = | 829.0 | nM | 6.08 |
| CHEMBL5189490 | — | IC50 | = | 825.0 | nM | 6.08 |
| CHEMBL5175755 | — | IC50 | = | 911.0 | nM | 6.04 |
| CHEMBL5171421 | — | IC50 | = | 991.0 | nM | 6.00 |
| CHEMBL5172719 | — | IC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL5209268 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL5207086 | — | IC50 | = | 1280.0 | nM | 5.89 |
| CHEMBL5183215 | — | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL5196851 | — | IC50 | = | 1430.0 | nM | 5.84 |
| CHEMBL5196480 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL5184295 | — | IC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL5174182 | — | IC50 | = | 1670.0 | nM | 5.78 |
| CHEMBL5196935 | — | IC50 | = | 1646.0 | nM | 5.78 |
| CHEMBL5205997 | — | IC50 | = | 1790.0 | nM | 5.75 |
| CHEMBL5196539 | — | IC50 | = | 1860.0 | nM | 5.73 |
| CHEMBL5173590 | — | IC50 | = | 1950.0 | nM | 5.71 |
| CHEMBL5200339 | — | IC50 | = | 2120.0 | nM | 5.67 |
| CHEMBL5170006 | — | IC50 | = | 2750.0 | nM | 5.56 |
| CHEMBL5203289 | — | IC50 | = | 3110.0 | nM | 5.51 |
| CHEMBL5177397 | — | IC50 | = | 3980.0 | nM | 5.40 |
| CHEMBL5187986 | — | IC50 | = | 4580.0 | nM | 5.34 |
| CHEMBL5178231 | — | IC50 | = | 4530.0 | nM | 5.34 |
| CHEMBL5176293 | — | IC50 | = | 4640.0 | nM | 5.33 |
| CHEMBL5205122 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5197514 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5198677 | — | IC50 | > | 10000.0 | nM | - |