Assay Detail
Binding
CHEMBL5155264
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kgamma (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
53
Total Activities
53
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 gamma isoform (CHEMBL3267) ↗| 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 | 53 | 8.53 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5171421 | — | — | 1 | 9.10 |
| CHEMBL5174699 | — | — | 1 | 9.10 |
| CHEMBL5179088 | — | — | 1 | 9.05 |
| CHEMBL5206549 | — | — | 1 | 9.05 |
| CHEMBL5186057 | — | — | 1 | 8.92 |
| CHEMBL5171703 | — | — | 1 | 8.89 |
| CHEMBL5182329 | — | — | 1 | 8.77 |
| CHEMBL5187986 | — | — | 1 | 8.77 |
| CHEMBL5200339 | — | — | 1 | 8.74 |
| CHEMBL5177379 | — | — | 1 | 8.74 |
| CHEMBL5203565 | — | — | 1 | 8.74 |
| CHEMBL5172570 | — | — | 1 | 8.74 |
| CHEMBL5209268 | — | — | 1 | 8.72 |
| CHEMBL5190157 | — | — | 1 | 8.72 |
| CHEMBL5178231 | — | — | 1 | 8.70 |
| CHEMBL5204993 | — | — | 1 | 8.68 |
| CHEMBL5172719 | — | — | 1 | 8.68 |
| CHEMBL5184295 | — | — | 1 | 8.64 |
| CHEMBL5196851 | — | — | 1 | 8.62 |
| CHEMBL5202602 | — | — | 1 | 8.62 |
| CHEMBL5177397 | — | — | 1 | 8.60 |
| CHEMBL5204743 | — | — | 1 | 8.57 |
| CHEMBL5194953 | — | — | 1 | 8.57 |
| CHEMBL5205997 | — | — | 1 | 8.55 |
| CHEMBL5196935 | — | — | 1 | 8.55 |
| CHEMBL4755842 | — | — | 1 | 8.54 |
| CHEMBL5205122 | — | — | 1 | 8.54 |
| CHEMBL5194457 | — | — | 1 | 8.52 |
| CHEMBL5201323 | — | — | 1 | 8.52 |
| CHEMBL5203289 | — | — | 1 | 8.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5171421 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5174699 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5206549 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5179088 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5186057 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5171703 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5182329 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5187986 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5200339 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5177379 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5203565 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5172570 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5209268 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5190157 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5178231 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5204993 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5172719 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5184295 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5196851 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5202602 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5177397 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5204743 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL5194953 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL5205997 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5196935 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4755842 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5205122 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5194457 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5201323 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5203289 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5176293 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5186453 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL5183215 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL5202984 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL5201929 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL5207086 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL5189490 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL5174182 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5173590 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5196539 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5172752 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL5200068 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5206156 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5196480 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL5171652 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL5197514 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL5173627 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL5182177 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL5170006 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL4740608 | — | IC50 | = | 9.1 | nM | 8.04 |