Assay Detail
Binding
CHEMBL4385118
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Inhibition of PI3Kbeta (unknown origin) using PIP2 as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by HTRF method
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (CHEMBL3145) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase δ through a Deconstruction and Regrowth Approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.73 | 6.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4466854 | — | — | 1 | 6.90 |
| CHEMBL4462877 | — | — | 1 | 6.80 |
| CHEMBL4469876 | — | — | 1 | 6.40 |
| CHEMBL4476588 | — | — | 1 | 6.30 |
| CHEMBL4474208 | — | — | 1 | 6.10 |
| CHEMBL4435246 | — | — | 1 | 6.00 |
| CHEMBL2216859 | NEMIRALISIB | 2.0 | 1 | 5.80 |
| CHEMBL4438305 | — | — | 1 | 5.60 |
| CHEMBL4434674 | — | — | 1 | 5.60 |
| CHEMBL4437969 | — | — | 1 | 5.40 |
| CHEMBL4468849 | — | — | 1 | 5.10 |
| CHEMBL4555426 | — | — | 1 | 4.80 |
| CHEMBL4580395 | — | — | 1 | 4.80 |
| CHEMBL4449676 | — | — | 1 | 4.60 |
| CHEMBL4590704 | — | — | 1 | - |
| CHEMBL4552815 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4466854 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL4462877 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4469876 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL4476588 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL4474208 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL4435246 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2216859 | NEMIRALISIB | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4438305 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL4434674 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL4437969 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL4468849 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL4555426 | — | IC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL4580395 | — | IC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL4449676 | — | IC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL4590704 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4552815 | — | IC50 | > | 50118.72 | nM | - |