Assay Detail
Binding
CHEMBL2173754
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal polyHis-tagged PI3K p110gamma expressed in baculovirus infected Hi5 cells using ATP as substrate after 20 mins by spectrophotometric analysis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BTI-TN-5B1-4 |
| 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
Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 7.78 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2170081 | — | — | 1 | 9.00 |
| CHEMBL2170098 | — | — | 1 | 8.15 |
| CHEMBL2170099 | — | — | 1 | 8.15 |
| CHEMBL2165017 | — | — | 1 | 8.10 |
| CHEMBL2170088 | — | — | 1 | 8.10 |
| CHEMBL2170083 | — | — | 1 | 8.05 |
| CHEMBL2170082 | — | — | 1 | 8.05 |
| CHEMBL2170089 | — | — | 1 | 8.05 |
| CHEMBL2170090 | — | — | 1 | 8.05 |
| CHEMBL2170087 | — | — | 1 | 7.92 |
| CHEMBL2170086 | — | — | 1 | 7.92 |
| CHEMBL2170095 | — | — | 1 | 7.80 |
| CHEMBL2170084 | — | — | 1 | 7.70 |
| CHEMBL2170096 | — | — | 1 | 7.68 |
| CHEMBL2170092 | — | — | 1 | 7.68 |
| CHEMBL2170097 | — | — | 1 | 7.62 |
| CHEMBL2170093 | — | — | 1 | 7.51 |
| CHEMBL2170085 | — | — | 1 | 7.47 |
| CHEMBL2170094 | — | — | 1 | 6.87 |
| CHEMBL2170091 | — | — | 1 | 5.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2170081 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL2170098 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL2170099 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL2165017 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL2170088 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL2170083 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL2170082 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL2170089 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL2170090 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL2170087 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL2170086 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL2170095 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2170084 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL2170096 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL2170092 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL2170097 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL2170093 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL2170085 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL2170094 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL2170091 | — | Ki | = | 2350.0 | nM | 5.63 |