Assay Detail
Binding
CHEMBL2157137
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Inhibition of human PI3Kgamma expressed in C5a-stimulated mouse RAW 264.7 cells assessed as inhibition of AKT phosphorylation by ELISA
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | RAW |
| 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 a novel series of potent and orally bioavailable phosphoinositide 3-kinase γ inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.30 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2152130 | — | — | 1 | 7.16 |
| CHEMBL2152141 | — | — | 1 | 6.77 |
| CHEMBL2152126 | — | — | 1 | 6.74 |
| CHEMBL2152144 | — | — | 1 | 6.74 |
| CHEMBL2152127 | — | — | 1 | 6.67 |
| CHEMBL2151050 | — | — | 1 | 6.58 |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 6.53 |
| CHEMBL2152129 | — | — | 1 | 6.49 |
| CHEMBL2152146 | — | — | 1 | 6.41 |
| CHEMBL2152147 | — | — | 1 | 6.39 |
| CHEMBL2152142 | — | — | 1 | 6.37 |
| CHEMBL2152150 | — | — | 1 | 6.33 |
| CHEMBL2152145 | — | — | 1 | 6.29 |
| CHEMBL2152148 | — | — | 1 | 6.28 |
| CHEMBL2152143 | — | — | 1 | 6.26 |
| CHEMBL2152140 | — | — | 1 | 6.24 |
| CHEMBL2152250 | — | — | 1 | 6.23 |
| CHEMBL2152252 | — | — | 1 | 6.11 |
| CHEMBL2152253 | — | — | 1 | 6.09 |
| CHEMBL2152149 | — | — | 1 | 5.80 |
| CHEMBL2152251 | — | — | 1 | 5.73 |
| CHEMBL2152124 | — | — | 1 | 5.44 |
| CHEMBL2152128 | — | — | 1 | 5.26 |
| CHEMBL2152125 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2152130 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL2152141 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL2152126 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL2152144 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL2152127 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL2151050 | — | IC50 | = | 264.0 | nM | 6.58 |
| CHEMBL521851 | PICTILISIB | IC50 | = | 298.0 | nM | 6.53 |
| CHEMBL2152129 | — | IC50 | = | 326.0 | nM | 6.49 |
| CHEMBL2152146 | — | IC50 | = | 394.0 | nM | 6.41 |
| CHEMBL2152147 | — | IC50 | = | 409.0 | nM | 6.39 |
| CHEMBL2152142 | — | IC50 | = | 431.0 | nM | 6.37 |
| CHEMBL2152150 | — | IC50 | = | 464.0 | nM | 6.33 |
| CHEMBL2152145 | — | IC50 | = | 507.0 | nM | 6.29 |
| CHEMBL2152148 | — | IC50 | = | 528.0 | nM | 6.28 |
| CHEMBL2152143 | — | IC50 | = | 552.0 | nM | 6.26 |
| CHEMBL2152140 | — | IC50 | = | 572.0 | nM | 6.24 |
| CHEMBL2152250 | — | IC50 | = | 587.0 | nM | 6.23 |
| CHEMBL2152252 | — | IC50 | = | 773.0 | nM | 6.11 |
| CHEMBL2152253 | — | IC50 | = | 805.0 | nM | 6.09 |
| CHEMBL2152149 | — | IC50 | = | 1575.0 | nM | 5.80 |
| CHEMBL2152251 | — | IC50 | = | 1877.0 | nM | 5.73 |
| CHEMBL2152124 | — | IC50 | = | 3608.0 | nM | 5.44 |
| CHEMBL2152128 | — | IC50 | = | 5430.0 | nM | 5.26 |
| CHEMBL2152125 | — | IC50 | > | 10000.0 | nM | - |