Assay Detail
ADMET
CHEMBL4828189
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal His6-tagged full length P110alpha/full length untagged human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by HTRF assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of GSK251: A Highly Potent, Highly Selective, Orally Bioavailable Inhibitor of PI3Kδ with a Novel Binding Mode.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 5.68 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4869356 | — | — | 1 | 6.60 |
| CHEMBL4845674 | — | — | 1 | 6.50 |
| CHEMBL4858875 | — | — | 1 | 6.50 |
| CHEMBL4850297 | — | — | 1 | 6.40 |
| CHEMBL4868232 | — | — | 1 | 6.30 |
| CHEMBL4175571 | — | — | 1 | 6.10 |
| CHEMBL4167702 | — | — | 1 | 6.00 |
| CHEMBL4870970 | — | — | 1 | 6.00 |
| CHEMBL4869783 | — | — | 1 | 6.00 |
| CHEMBL4175737 | — | — | 1 | 5.90 |
| CHEMBL4170075 | — | — | 1 | 5.90 |
| CHEMBL4855234 | — | — | 1 | 5.90 |
| CHEMBL4873390 | — | — | 1 | 5.90 |
| CHEMBL4870020 | — | — | 1 | 5.80 |
| CHEMBL4173087 | — | — | 1 | 5.80 |
| CHEMBL4877869 | — | — | 1 | 5.80 |
| CHEMBL4469876 | — | — | 1 | 5.70 |
| CHEMBL4174874 | — | — | 1 | 5.60 |
| CHEMBL4169192 | — | — | 1 | 5.60 |
| CHEMBL4867203 | — | — | 1 | 5.50 |
| CHEMBL4859024 | — | — | 1 | 5.50 |
| CHEMBL4849115 | — | — | 1 | 5.40 |
| CHEMBL4876289 | — | — | 1 | 5.40 |
| CHEMBL4870356 | — | — | 1 | 5.40 |
| CHEMBL4846241 | — | — | 1 | 5.30 |
| CHEMBL4872328 | — | — | 1 | 5.30 |
| CHEMBL4869306 | — | — | 1 | 5.30 |
| CHEMBL4868553 | — | — | 1 | 5.30 |
| CHEMBL4863100 | — | — | 1 | 5.30 |
| CHEMBL4872822 | — | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4869356 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL4845674 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL4858875 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL4850297 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL4868232 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL4175571 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL4167702 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4870970 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4869783 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4175737 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL4170075 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL4855234 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL4873390 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL4877869 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4173087 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4870020 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4469876 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL4174874 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL4169192 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL4867203 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL4859024 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL4849115 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL4876289 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL4870356 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL4846241 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL4872328 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL4869306 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL4868553 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL4863100 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL4872822 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL4878870 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL4877995 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL4852717 | — | IC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL4857056 | — | IC50 | = | 19952.62 | nM | 4.70 |