Assay Detail
Binding
CHEMBL4385718
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Inhibition of His-tagged recombinant human PI3K p110delta/p85alpha using lipid substrate incubated for 2 hrs by ADP-Glo assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.20 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2216870 | IDELALISIB | 4.0 | 1 | 8.74 |
| CHEMBL4471679 | — | — | 1 | 8.49 |
| CHEMBL4468379 | — | — | 1 | 8.34 |
| CHEMBL4471020 | — | — | 1 | 8.15 |
| CHEMBL4557623 | — | — | 1 | 8.01 |
| CHEMBL4465593 | — | — | 1 | 7.92 |
| CHEMBL573339 | PI-103 | — | 1 | 7.85 |
| CHEMBL4533033 | — | — | 1 | 7.82 |
| CHEMBL4438104 | — | — | 1 | 7.46 |
| CHEMBL4457627 | — | — | 1 | 7.27 |
| CHEMBL4520088 | — | — | 1 | 7.21 |
| CHEMBL4513312 | — | — | 1 | 7.17 |
| CHEMBL4467198 | — | — | 1 | 7.09 |
| CHEMBL4475921 | — | — | 1 | 7.04 |
| CHEMBL4550989 | — | — | 1 | 6.85 |
| CHEMBL4441846 | — | — | 1 | 6.46 |
| CHEMBL4439236 | — | — | 1 | 6.42 |
| CHEMBL4476052 | — | — | 1 | 6.21 |
| CHEMBL4543408 | — | — | 1 | 6.20 |
| CHEMBL4560275 | — | — | 1 | 6.04 |
| CHEMBL4537510 | — | — | 1 | 5.92 |
| CHEMBL4451945 | — | — | 1 | 5.70 |
| CHEMBL4441934 | — | — | 1 | - |
| CHEMBL4569683 | — | — | 1 | - |
| CHEMBL4455854 | — | — | 1 | - |
| CHEMBL4572206 | — | — | 1 | - |
| CHEMBL4465857 | — | — | 1 | - |
| CHEMBL4444852 | — | — | 1 | - |
| CHEMBL4453364 | — | — | 1 | - |
| CHEMBL4539820 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2216870 | IDELALISIB | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4471679 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4468379 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4471020 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4557623 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL4465593 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL573339 | PI-103 | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4533033 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4438104 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4457627 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4520088 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4513312 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4467198 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4475921 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4550989 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL4441846 | — | IC50 | = | 344.0 | nM | 6.46 |
| CHEMBL4439236 | — | IC50 | = | 383.0 | nM | 6.42 |
| CHEMBL4476052 | — | IC50 | = | 623.0 | nM | 6.21 |
| CHEMBL4543408 | — | IC50 | = | 628.0 | nM | 6.20 |
| CHEMBL4560275 | — | IC50 | = | 921.0 | nM | 6.04 |
| CHEMBL4537510 | — | IC50 | = | 1202.0 | nM | 5.92 |
| CHEMBL4451945 | — | IC50 | = | 1999.0 | nM | 5.70 |
| CHEMBL4441934 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4569683 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4455854 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4572206 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4465857 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4444852 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4453364 | — | IC50 | < | 0.32 | nM | - |
| CHEMBL4539820 | — | IC50 | > | 3000.0 | nM | - |