Assay Detail
ADMET
CHEMBL4124221
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Inhibition of recombinant human 6His-tagged PI3K p110alpha/p85alpha using DiC8-PIP2 as substrate preincubated for 10 mins followed by substrate addition measured after 60 mins by ADP-Glo assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| 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 | 18 | 5.34 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4127150 | — | — | 1 | 7.10 |
| CHEMBL4127833 | — | — | 1 | 5.60 |
| CHEMBL4126601 | — | — | 1 | 5.60 |
| CHEMBL4126445 | — | — | 1 | 5.50 |
| CHEMBL4129600 | — | — | 1 | 5.40 |
| CHEMBL4126010 | — | — | 1 | 5.30 |
| CHEMBL4130021 | — | — | 1 | 5.20 |
| CHEMBL4128537 | — | — | 1 | 5.20 |
| CHEMBL4127396 | — | — | 1 | 5.20 |
| CHEMBL4126156 | — | — | 1 | 5.10 |
| CHEMBL4129457 | — | — | 1 | 5.10 |
| CHEMBL4129877 | — | — | 1 | 5.00 |
| CHEMBL4128230 | — | — | 1 | 4.90 |
| CHEMBL4128652 | — | — | 1 | 4.60 |
| CHEMBL4128809 | — | — | 1 | - |
| CHEMBL4127414 | — | — | 1 | - |
| CHEMBL4129270 | — | — | 1 | - |
| CHEMBL4125955 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4127150 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL4127833 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL4126601 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL4126445 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL4129600 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL4126010 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL4130021 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL4128537 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL4127396 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL4126156 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL4129457 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL4129877 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4128230 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL4128652 | — | IC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL4128809 | — | IC50 | > | 31622.78 | nM | - |
| CHEMBL4127414 | — | IC50 | > | 31622.78 | nM | - |
| CHEMBL4129270 | — | IC50 | > | 31622.78 | nM | - |
| CHEMBL4125955 | — | IC50 | > | 31622.78 | nM | - |