Assay Detail
Binding
CHEMBL895750
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Inhibition of recombinant PI3Kgamma
30
Total Activities
30
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (CHEMBL3267) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 3,3'-(2,4-diaminopteridine-6,7-diyl)diphenol as an isozyme-selective inhibitor of PI3K for the treatment of ischemia reperfusion injury associated with myocardial infarction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 5.62 | 7.90 |
| Activity | 8 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL230098 | — | — | 1 | 7.90 |
| CHEMBL244559 | — | — | 1 | 7.40 |
| CHEMBL230011 | TG100-115 | 2.0 | 1 | 7.08 |
| CHEMBL243506 | — | — | 1 | 6.71 |
| CHEMBL397925 | — | — | 1 | 6.56 |
| CHEMBL1162956 | — | — | 1 | 6.01 |
| CHEMBL397902 | — | — | 1 | 5.92 |
| CHEMBL397737 | — | — | 1 | 5.89 |
| CHEMBL395726 | — | — | 1 | 5.57 |
| CHEMBL242429 | — | — | 1 | 5.52 |
| CHEMBL437543 | — | — | 1 | 5.40 |
| CHEMBL231581 | — | — | 1 | 5.40 |
| CHEMBL441318 | — | — | 1 | 5.33 |
| CHEMBL230647 | — | — | 1 | 5.29 |
| CHEMBL244570 | — | — | 1 | 5.23 |
| CHEMBL48296 | — | — | 1 | 5.07 |
| CHEMBL390209 | — | — | 1 | 5.05 |
| CHEMBL243064 | — | — | 1 | 4.77 |
| CHEMBL389541 | — | — | 1 | 4.49 |
| CHEMBL388946 | — | — | 1 | 4.34 |
| CHEMBL244552 | — | — | 1 | 4.32 |
| CHEMBL244770 | — | — | 1 | 4.29 |
| CHEMBL230646 | — | — | 1 | - |
| CHEMBL244349 | — | — | 1 | - |
| CHEMBL230547 | — | — | 1 | - |
| CHEMBL230546 | — | — | 1 | - |
| CHEMBL244558 | — | — | 1 | - |
| CHEMBL231163 | — | — | 1 | - |
| CHEMBL230437 | — | — | 1 | - |
| CHEMBL244352 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL230098 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL244559 | — | IC50 | = | 39.9 | nM | 7.40 |
| CHEMBL230011 | TG100-115 | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL243506 | — | IC50 | = | 195.0 | nM | 6.71 |
| CHEMBL397925 | — | IC50 | = | 273.0 | nM | 6.56 |
| CHEMBL1162956 | — | IC50 | = | 968.0 | nM | 6.01 |
| CHEMBL397902 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL397737 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL395726 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL242429 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL437543 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL231581 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL441318 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL230647 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL244570 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL48296 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL390209 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL243064 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL389541 | — | IC50 | = | 32700.0 | nM | 4.49 |
| CHEMBL388946 | — | IC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL244552 | — | IC50 | = | 48000.0 | nM | 4.32 |
| CHEMBL244770 | — | IC50 | = | 51000.0 | nM | 4.29 |
| CHEMBL230646 | — | Activity | - | — | - | |
| CHEMBL244349 | — | Activity | - | — | - | |
| CHEMBL230547 | — | Activity | - | — | - | |
| CHEMBL230546 | — | Activity | - | — | - | |
| CHEMBL244558 | — | Activity | - | — | - | |
| CHEMBL231163 | — | Activity | - | — | - | |
| CHEMBL230437 | — | Activity | - | — | - | |
| CHEMBL244352 | — | Activity | - | — | - |