Assay Detail
Binding
CHEMBL5587987
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3K alpha (unknown origin) using PI3:PS as substrate incubated for 1 hr in presence of ATP by ADP-glo kinase assay
35
Total Activities
35
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 alpha isoform (CHEMBL4005) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Pyrazolo[1,5-<i>a</i>]pyridine Derivatives as Potent and Selective PI3Kγ/δ Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 7.03 | 8.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5597293 | — | — | 1 | 8.44 |
| CHEMBL5598183 | — | — | 1 | 8.43 |
| CHEMBL5590113 | — | — | 1 | 8.42 |
| CHEMBL5597159 | — | — | 1 | 8.38 |
| CHEMBL5596579 | — | — | 1 | 8.37 |
| CHEMBL5597286 | — | — | 1 | 8.35 |
| CHEMBL5597786 | — | — | 1 | 8.34 |
| CHEMBL5596957 | — | — | 1 | 8.10 |
| CHEMBL5597639 | — | — | 1 | 8.08 |
| CHEMBL5597160 | — | — | 1 | 7.94 |
| CHEMBL5596755 | — | — | 1 | 7.87 |
| CHEMBL5597322 | — | — | 1 | 7.85 |
| CHEMBL5596364 | — | — | 1 | 7.73 |
| CHEMBL5596530 | — | — | 1 | 7.64 |
| CHEMBL5598309 | — | — | 1 | 7.63 |
| CHEMBL5598454 | — | — | 1 | 6.90 |
| CHEMBL5596470 | — | — | 1 | 6.90 |
| CHEMBL5590633 | — | — | 1 | 6.88 |
| CHEMBL5598560 | — | — | 1 | 6.87 |
| CHEMBL5596114 | — | — | 1 | 6.53 |
| CHEMBL5596611 | — | — | 1 | 6.45 |
| CHEMBL5590382 | — | — | 1 | 6.00 |
| CHEMBL5596735 | — | — | 1 | 5.59 |
| CHEMBL5597903 | — | — | 1 | 5.58 |
| CHEMBL5596701 | — | — | 1 | 5.43 |
| CHEMBL5597610 | — | — | 1 | 5.38 |
| CHEMBL5598104 | — | — | 1 | 5.30 |
| CHEMBL5596396 | — | — | 1 | 5.18 |
| CHEMBL5596348 | — | — | 1 | 5.12 |
| CHEMBL5597669 | — | — | 1 | 5.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5597293 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5598183 | — | IC50 | = | 3.71 | nM | 8.43 |
| CHEMBL5590113 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL5597159 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5596579 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL5597286 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL5597786 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL5596957 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL5597639 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL5597160 | — | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL5596755 | — | IC50 | = | 13.6 | nM | 7.87 |
| CHEMBL5597322 | — | IC50 | = | 14.2 | nM | 7.85 |
| CHEMBL5596364 | — | IC50 | = | 18.8 | nM | 7.73 |
| CHEMBL5596530 | — | IC50 | = | 22.8 | nM | 7.64 |
| CHEMBL5598309 | — | IC50 | = | 23.4 | nM | 7.63 |
| CHEMBL5598454 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL5596470 | — | IC50 | = | 125.6 | nM | 6.90 |
| CHEMBL5590633 | — | IC50 | = | 131.8 | nM | 6.88 |
| CHEMBL5598560 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL5596114 | — | IC50 | = | 297.0 | nM | 6.53 |
| CHEMBL5596611 | — | IC50 | = | 354.7 | nM | 6.45 |
| CHEMBL5590382 | — | IC50 | = | 994.0 | nM | 6.00 |
| CHEMBL5596735 | — | IC50 | = | 2573.0 | nM | 5.59 |
| CHEMBL5597903 | — | IC50 | = | 2654.0 | nM | 5.58 |
| CHEMBL5596701 | — | IC50 | = | 3731.0 | nM | 5.43 |
| CHEMBL5597610 | — | IC50 | = | 4146.0 | nM | 5.38 |
| CHEMBL5598104 | — | IC50 | = | 4979.0 | nM | 5.30 |
| CHEMBL5596396 | — | IC50 | = | 6617.0 | nM | 5.18 |
| CHEMBL5596348 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL5597669 | — | IC50 | = | 7552.0 | nM | 5.12 |
| CHEMBL5597218 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5591103 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5597788 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5596476 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5597371 | — | IC50 | > | 10000.0 | nM | - |