Assay Detail
Binding
CHEMBL4124223
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Inhibition of recombinant human 6His-tagged PI3K p110delta/p85alpha using DiC8-PIP2 as substrate preincubated for 10 mins followed by substrate addition measured after 60 mins by ADP-Glo assay
16
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3-Kinase (PI3K)-γ Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.25 | 6.80 |
| pIC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4129600 | — | — | 1 | 6.80 |
| CHEMBL4126445 | — | — | 1 | 6.70 |
| CHEMBL4129457 | — | — | 1 | 6.70 |
| CHEMBL4127150 | — | — | 1 | 6.60 |
| CHEMBL4128537 | — | — | 1 | 6.60 |
| CHEMBL4127396 | — | — | 1 | 6.60 |
| CHEMBL4126010 | — | — | 1 | 6.60 |
| CHEMBL4126601 | — | — | 1 | 6.50 |
| CHEMBL4126156 | — | — | 1 | 6.50 |
| CHEMBL4128230 | — | — | 1 | 6.40 |
| CHEMBL4127833 | — | — | 1 | 6.30 |
| CHEMBL4129877 | — | — | 1 | 5.80 |
| CHEMBL4130021 | — | — | 1 | 5.50 |
| CHEMBL4128652 | — | — | 1 | 5.20 |
| CHEMBL4128809 | — | — | 1 | 5.00 |
| CHEMBL4127414 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4129600 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4126445 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL4129457 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL4127150 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL4128537 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL4127396 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL4126010 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL4126601 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL4126156 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL4128230 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL4127833 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL4129877 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4130021 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL4128652 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL4128809 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4127414 | — | pIC50 | - | — | - |