Assay Detail
Functional
CHEMBL4724075
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Anticancer activity against human TMD8 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | TMD8 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of a Potent and Selective PI3Kδ Inhibitor (S)-2,4-Diamino-6-((1-(7-fluoro-1-(4-fluorophenyl)-4-oxo-3-phenyl-4H-quinolizin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile with Improved Pharmacokinetic Profile and Superior Efficacy in Hematological Cancer Models.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 9.40 | 10.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4749521 | — | — | 1 | 10.92 |
| CHEMBL4463183 | — | — | 1 | 10.10 |
| CHEMBL4794328 | — | — | 1 | 10.05 |
| CHEMBL2216870 | IDELALISIB | 4.0 | 1 | 8.14 |
| CHEMBL4755417 | — | — | 1 | 7.80 |
| CHEMBL4756563 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4749521 | — | IC50 | = | 0.012 | nM | 10.92 |
| CHEMBL4463183 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL4794328 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL2216870 | IDELALISIB | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL4755417 | — | IC50 | = | 15.91 | nM | 7.80 |
| CHEMBL4756563 | — | IC50 | < | 0.1 | nM | - |