Assay Detail
Functional
CHEMBL3738495
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Antiproliferative activity against ALK-dependent human NCI-H3122 cells after 72 hrs
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NCI-H3122 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Novel tetracyclic benzo[b]carbazolones as highly potent and orally bioavailable ALK inhibitors: design, synthesis, and structure-activity relationship study.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.46 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3735064 | — | — | 1 | 8.62 |
| CHEMBL3735587 | — | — | 1 | 8.57 |
| CHEMBL3735401 | — | — | 1 | 8.23 |
| CHEMBL3736021 | — | — | 1 | 7.82 |
| CHEMBL3735531 | — | — | 1 | 7.79 |
| CHEMBL3735648 | — | — | 1 | 7.75 |
| CHEMBL1738797 | ALECTINIB | 4.0 | 1 | 7.72 |
| CHEMBL3734938 | — | — | 1 | 7.70 |
| CHEMBL3734855 | — | — | 1 | 7.69 |
| CHEMBL3735794 | — | — | 1 | 7.60 |
| CHEMBL3736267 | — | — | 1 | 7.44 |
| CHEMBL3735386 | — | — | 1 | 7.31 |
| CHEMBL3736273 | — | — | 1 | 7.22 |
| CHEMBL3735510 | — | — | 1 | 7.16 |
| CHEMBL3735314 | — | — | 1 | 7.16 |
| CHEMBL3736388 | — | — | 1 | 6.90 |
| CHEMBL3735650 | — | — | 1 | 6.76 |
| CHEMBL3735384 | — | — | 1 | 6.73 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.58 |
| CHEMBL3736182 | — | — | 1 | 6.51 |
| CHEMBL3735980 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3735064 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3735587 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3735401 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL3736021 | — | IC50 | = | 15.3 | nM | 7.82 |
| CHEMBL3735531 | — | IC50 | = | 16.3 | nM | 7.79 |
| CHEMBL3735648 | — | IC50 | = | 17.9 | nM | 7.75 |
| CHEMBL1738797 | ALECTINIB | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3734938 | — | IC50 | = | 19.9 | nM | 7.70 |
| CHEMBL3734855 | — | IC50 | = | 20.6 | nM | 7.69 |
| CHEMBL3735794 | — | IC50 | = | 24.9 | nM | 7.60 |
| CHEMBL3736267 | — | IC50 | = | 36.4 | nM | 7.44 |
| CHEMBL3735386 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL3736273 | — | IC50 | = | 59.6 | nM | 7.22 |
| CHEMBL3735510 | — | IC50 | = | 69.1 | nM | 7.16 |
| CHEMBL3735314 | — | IC50 | = | 69.6 | nM | 7.16 |
| CHEMBL3736388 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL3735650 | — | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL3735384 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 261.2 | nM | 6.58 |
| CHEMBL3736182 | — | IC50 | = | 309.0 | nM | 6.51 |
| CHEMBL3735980 | — | IC50 | > | 2000.0 | nM | - |