Assay Detail
Binding
CHEMBL4670194
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kgamma in human THP-1 cells assessed as reduction in Akt phosphorylation at S473 residue incubated for 60 mins by alphalisa assay
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | THP-1 |
| 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
Discovery of Potent and Selective PI3Kγ Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 6.20 | 7.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4782083 | — | — | 1 | 7.19 |
| CHEMBL4742062 | — | — | 1 | 7.13 |
| CHEMBL4740423 | — | — | 1 | 7.12 |
| CHEMBL4126445 | — | — | 1 | 7.06 |
| CHEMBL4785086 | — | — | 1 | 6.82 |
| CHEMBL4778393 | — | — | 1 | 6.80 |
| CHEMBL4755842 | — | — | 1 | 6.70 |
| CHEMBL4762555 | — | — | 1 | 6.68 |
| CHEMBL4779748 | — | — | 1 | 6.64 |
| CHEMBL4784554 | — | — | 1 | 6.62 |
| CHEMBL4759380 | — | — | 1 | 6.62 |
| CHEMBL4740608 | — | — | 1 | 6.52 |
| CHEMBL4798877 | — | — | 1 | 6.40 |
| CHEMBL4752240 | — | — | 1 | 6.36 |
| CHEMBL4740304 | — | — | 1 | 6.36 |
| CHEMBL4764627 | — | — | 1 | 6.35 |
| CHEMBL4789901 | — | — | 1 | 6.34 |
| CHEMBL4761503 | — | — | 1 | 6.33 |
| CHEMBL4782224 | — | — | 1 | 6.31 |
| CHEMBL4783357 | — | — | 1 | 6.26 |
| CHEMBL4745355 | — | — | 1 | 6.21 |
| CHEMBL4740456 | — | — | 1 | 6.20 |
| CHEMBL4755285 | — | — | 1 | 6.16 |
| CHEMBL4749404 | — | — | 1 | 6.10 |
| CHEMBL4792935 | — | — | 1 | 6.08 |
| CHEMBL4743121 | — | — | 1 | 6.06 |
| CHEMBL4746190 | — | — | 1 | 6.00 |
| CHEMBL4743136 | — | — | 1 | 5.82 |
| CHEMBL4764239 | — | — | 1 | 5.82 |
| CHEMBL4752498 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4782083 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4742062 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4740423 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4126445 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4785086 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4778393 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4755842 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4762555 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4779748 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4784554 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4759380 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4740608 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4798877 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4752240 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4740304 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4764627 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4789901 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL4761503 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4782224 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4783357 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4745355 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL4740456 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL4755285 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL4749404 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL4792935 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL4743121 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL4746190 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4743136 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4764239 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4752498 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4791781 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4752359 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4793165 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4797944 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL4742806 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL4744486 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4746682 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL4794833 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4762674 | — | IC50 | - | — | - |