Assay Detail
Binding
CHEMBL2173755
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Inhibition of human N-terminal polyHis-tagged PI3K p110beta/p85alpha expressed in baculovirus infected Sf9 cells using phosphatidylinositol-4,5-bisphosphate 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 | Sf9 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
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 | 7.91 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2170090 | — | — | 1 | 8.70 |
| CHEMBL2170089 | — | — | 1 | 8.70 |
| CHEMBL2170099 | — | — | 1 | 8.52 |
| CHEMBL2170088 | — | — | 1 | 8.52 |
| CHEMBL2170082 | — | — | 1 | 8.40 |
| CHEMBL2165017 | — | — | 1 | 8.30 |
| CHEMBL2170083 | — | — | 1 | 8.30 |
| CHEMBL2170086 | — | — | 1 | 8.22 |
| CHEMBL2170081 | — | — | 1 | 8.22 |
| CHEMBL2170087 | — | — | 1 | 8.10 |
| CHEMBL2170096 | — | — | 1 | 8.10 |
| CHEMBL2170095 | — | — | 1 | 8.00 |
| CHEMBL2170084 | — | — | 1 | 7.92 |
| CHEMBL2170092 | — | — | 1 | 7.77 |
| CHEMBL2170097 | — | — | 1 | 7.72 |
| CHEMBL2170093 | — | — | 1 | 7.70 |
| CHEMBL2170085 | — | — | 1 | 7.68 |
| CHEMBL2170098 | — | — | 1 | 7.26 |
| CHEMBL2170094 | — | — | 1 | 6.84 |
| CHEMBL2170091 | — | — | 1 | 5.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2170090 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL2170089 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL2170099 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL2170088 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL2170082 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL2165017 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2170083 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2170086 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL2170081 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL2170087 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL2170096 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL2170095 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2170084 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL2170092 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL2170097 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL2170093 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL2170085 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL2170098 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL2170094 | — | Ki | = | 143.0 | nM | 6.84 |
| CHEMBL2170091 | — | Ki | = | 4810.0 | nM | 5.32 |