Assay Detail
Functional
CHEMBL904299
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Induction of apoptosis in human H1299 cells assessed as caspase activation after 24 hrs
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NCI-H1299 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 1. Structure-activity relationships of the 4-aryl group.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 44 | 6.45 | 7.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL223322 | — | — | 1 | 7.57 |
| CHEMBL107 | COLCHICINE | 4.0 | 1 | 7.47 |
| CHEMBL222919 | — | — | 1 | 7.47 |
| CHEMBL222048 | — | — | 1 | 7.44 |
| CHEMBL196832 | — | — | 1 | 7.37 |
| CHEMBL439139 | — | — | 1 | 7.34 |
| CHEMBL437934 | — | — | 1 | 7.20 |
| CHEMBL159 | VINBLASTINE | 4.0 | 1 | 7.14 |
| CHEMBL374886 | — | — | 1 | 7.14 |
| CHEMBL373137 | — | — | 1 | 7.03 |
| CHEMBL375231 | — | — | 1 | 6.94 |
| CHEMBL390502 | — | — | 1 | 6.84 |
| CHEMBL221995 | — | — | 1 | 6.81 |
| CHEMBL428647 | PACLITAXEL | 4.0 | 1 | 6.79 |
| CHEMBL387389 | — | — | 1 | 6.70 |
| CHEMBL375247 | — | — | 1 | 6.67 |
| CHEMBL225406 | — | — | 1 | 6.63 |
| CHEMBL374774 | — | — | 1 | 6.62 |
| CHEMBL225066 | — | — | 1 | 6.56 |
| CHEMBL221895 | — | — | 1 | 6.52 |
| CHEMBL222409 | — | — | 1 | 6.52 |
| CHEMBL221510 | — | — | 1 | 6.47 |
| CHEMBL225132 | — | — | 1 | 6.38 |
| CHEMBL225549 | — | — | 1 | 6.29 |
| CHEMBL221665 | — | — | 1 | 6.29 |
| CHEMBL446709 | — | — | 1 | 6.25 |
| CHEMBL223037 | — | — | 1 | 6.23 |
| CHEMBL223378 | — | — | 1 | 6.21 |
| CHEMBL225173 | — | — | 1 | 6.12 |
| CHEMBL427063 | — | — | 1 | 6.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL223322 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL107 | COLCHICINE | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL222919 | — | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL222048 | — | EC50 | = | 36.0 | nM | 7.44 |
| CHEMBL196832 | — | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL439139 | — | EC50 | = | 46.0 | nM | 7.34 |
| CHEMBL437934 | — | EC50 | = | 63.0 | nM | 7.20 |
| CHEMBL159 | VINBLASTINE | EC50 | = | 73.0 | nM | 7.14 |
| CHEMBL374886 | — | EC50 | = | 73.0 | nM | 7.14 |
| CHEMBL373137 | — | EC50 | = | 93.0 | nM | 7.03 |
| CHEMBL375231 | — | EC50 | = | 115.0 | nM | 6.94 |
| CHEMBL390502 | — | EC50 | = | 144.0 | nM | 6.84 |
| CHEMBL221995 | — | EC50 | = | 155.0 | nM | 6.81 |
| CHEMBL428647 | PACLITAXEL | EC50 | = | 163.0 | nM | 6.79 |
| CHEMBL387389 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL375247 | — | EC50 | = | 215.0 | nM | 6.67 |
| CHEMBL225406 | — | EC50 | = | 233.0 | nM | 6.63 |
| CHEMBL374774 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL225066 | — | EC50 | = | 277.0 | nM | 6.56 |
| CHEMBL221895 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL222409 | — | EC50 | = | 304.0 | nM | 6.52 |
| CHEMBL221510 | — | EC50 | = | 337.0 | nM | 6.47 |
| CHEMBL225132 | — | EC50 | = | 420.0 | nM | 6.38 |
| CHEMBL221665 | — | EC50 | = | 514.0 | nM | 6.29 |
| CHEMBL225549 | — | EC50 | = | 510.0 | nM | 6.29 |
| CHEMBL446709 | — | EC50 | = | 560.0 | nM | 6.25 |
| CHEMBL223037 | — | EC50 | = | 583.0 | nM | 6.23 |
| CHEMBL223378 | — | EC50 | = | 622.0 | nM | 6.21 |
| CHEMBL225173 | — | EC50 | = | 754.0 | nM | 6.12 |
| CHEMBL427063 | — | EC50 | = | 855.0 | nM | 6.07 |
| CHEMBL373475 | — | EC50 | = | 959.0 | nM | 6.02 |
| CHEMBL375289 | — | EC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL223428 | — | EC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL222981 | — | EC50 | = | 1430.0 | nM | 5.84 |
| CHEMBL225120 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL221509 | — | EC50 | = | 2130.0 | nM | 5.67 |
| CHEMBL375974 | — | EC50 | = | 2230.0 | nM | 5.65 |
| CHEMBL223036 | — | EC50 | = | 2290.0 | nM | 5.64 |
| CHEMBL374885 | — | EC50 | = | 3370.0 | nM | 5.47 |
| CHEMBL221997 | — | EC50 | = | 3560.0 | nM | 5.45 |
| CHEMBL222052 | — | EC50 | = | 3740.0 | nM | 5.43 |
| CHEMBL373734 | — | EC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL389916 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL373806 | — | EC50 | > | 10000.0 | nM | - |