Assay Detail
Functional
CHEMBL4428712
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Inhibition of cell proliferation of human B cells pre-incubated for 30 mins before anti-IgM/CD40L stimulation and measured after 72 hrs by [3H]thymidine incorporation assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | B cell |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-5-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-1430).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 8.75 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4443843 | — | — | 1 | 9.70 |
| CHEMBL4470291 | — | — | 1 | 9.10 |
| CHEMBL4449576 | — | — | 1 | 8.92 |
| CHEMBL4525494 | — | — | 1 | 8.92 |
| CHEMBL4464055 | — | — | 1 | 8.92 |
| CHEMBL4461539 | — | — | 1 | 8.89 |
| CHEMBL4572863 | — | — | 1 | 8.80 |
| CHEMBL4442808 | — | — | 1 | 8.80 |
| CHEMBL4555334 | — | — | 1 | 8.74 |
| CHEMBL4516601 | — | — | 1 | 8.72 |
| CHEMBL4570159 | — | — | 1 | 8.66 |
| CHEMBL4438514 | — | — | 1 | 8.54 |
| CHEMBL3403678 | — | — | 1 | 8.34 |
| CHEMBL4594095 | — | — | 1 | 8.13 |
| CHEMBL4303596 | AMG-319 | 2.0 | 1 | 8.07 |
| CHEMBL4449366 | — | — | 1 | - |
| CHEMBL4542785 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4443843 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4470291 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4449576 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4525494 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4464055 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4461539 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4572863 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4442808 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4555334 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4516601 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4570159 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4438514 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL3403678 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4594095 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL4303596 | AMG-319 | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL4449366 | — | IC50 | - | — | - | |
| CHEMBL4542785 | — | IC50 | - | — | - |