Assay Detail
Functional
CHEMBL2025199
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Inhibition of VEGF-A secretion in human HCT116 cells after 12 hrs
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HCT-116 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Systematic Chemical Mutagenesis Identifies a Potent Novel Apratoxin A/E Hybrid with Improved in Vivo Antitumor Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.41 | 9.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2022564 | APRATOXIN S4 | — | 1 | 9.51 |
| CHEMBL2022562 | APRATOXIN S2 | — | 1 | 9.49 |
| CHEMBL2022566 | APRATOXIN S6 | — | 1 | 9.41 |
| CHEMBL2022560 | APRATOXIN F | — | 1 | 9.34 |
| CHEMBL501696 | APRATOXIN A | — | 1 | 8.83 |
| CHEMBL506311 | APRATOXIN E | — | 1 | 8.04 |
| CHEMBL2022561 | APRATOXIN S1 | — | 1 | 7.68 |
| CHEMBL2022565 | APRATOXIN S5 | — | 1 | 6.95 |
| CHEMBL2022563 | APRATOXIN S3 | — | 1 | 6.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2022564 | APRATOXIN S4 | IC50 | = | 0.308 | nM | 9.51 |
| CHEMBL2022562 | APRATOXIN S2 | IC50 | = | 0.322 | nM | 9.49 |
| CHEMBL2022566 | APRATOXIN S6 | IC50 | = | 0.391 | nM | 9.41 |
| CHEMBL2022560 | APRATOXIN F | IC50 | = | 0.461 | nM | 9.34 |
| CHEMBL501696 | APRATOXIN A | IC50 | = | 1.49 | nM | 8.83 |
| CHEMBL506311 | APRATOXIN E | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL2022561 | APRATOXIN S1 | IC50 | = | 20.7 | nM | 7.68 |
| CHEMBL2022565 | APRATOXIN S5 | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL2022563 | APRATOXIN S3 | IC50 | = | 340.0 | nM | 6.47 |