Assay Detail
Functional
CHEMBL4733830
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Antiproliferative activity against human Rh30 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | SJRH30 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) as an orally bioavailable, highly potent, PI3K alpha inhibitor for the treatment of advanced solid tumors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.26 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4756324 | — | — | 1 | 7.16 |
| CHEMBL4742751 | — | — | 1 | 7.10 |
| CHEMBL4800181 | — | — | 1 | 7.05 |
| CHEMBL4784118 | — | — | 1 | 6.82 |
| CHEMBL4783228 | — | — | 1 | 6.75 |
| CHEMBL4756074 | — | — | 1 | 6.64 |
| CHEMBL4781518 | — | — | 1 | 6.41 |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 6.32 |
| CHEMBL4740055 | — | — | 1 | 6.15 |
| CHEMBL4761702 | — | — | 1 | 6.06 |
| CHEMBL4791280 | — | — | 1 | 6.01 |
| CHEMBL4800252 | RISOVALISIB | 2.0 | 1 | 5.99 |
| CHEMBL4799728 | — | — | 1 | 5.75 |
| CHEMBL4779801 | — | — | 1 | 5.49 |
| CHEMBL4760391 | — | — | 1 | 5.29 |
| CHEMBL2396661 | ALPELISIB | 4.0 | 1 | 5.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4756324 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4742751 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4800181 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4784118 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4783228 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4756074 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4781518 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL521851 | PICTILISIB | IC50 | = | 478.0 | nM | 6.32 |
| CHEMBL4740055 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL4761702 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL4791280 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL4800252 | RISOVALISIB | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL4799728 | — | IC50 | = | 1780.0 | nM | 5.75 |
| CHEMBL4779801 | — | IC50 | = | 3270.0 | nM | 5.49 |
| CHEMBL4760391 | — | IC50 | = | 5070.0 | nM | 5.29 |
| CHEMBL2396661 | ALPELISIB | IC50 | = | 7600.0 | nM | 5.12 |