Assay Detail
Binding
CHEMBL1243914
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Inhibition of SAP130 in VEGF-stimulated human U251 cells by PLAP reporter gene assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U-251 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Splicing factor SF3b as a target of the antitumor natural product pladienolide.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.27 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1242745 | PLADIENOLIDE B | — | 1 | 8.89 |
| CHEMBL1242564 | PLA D | — | 1 | 8.48 |
| CHEMBL1240972 | — | — | 1 | 8.44 |
| CHEMBL1242467 | PLADIENOLIDE C | — | 1 | 8.30 |
| CHEMBL1242284 | — | — | 1 | 8.18 |
| CHEMBL269732 | TACROLIMUS ANHYDROUS | 4.0 | 1 | 7.86 |
| CHEMBL1242654 | PLADIENOLIDE E | — | 1 | 7.23 |
| CHEMBL1240973 | — | — | 1 | 7.11 |
| CHEMBL1242841 | PLADIENOLIDE A | — | 1 | 6.51 |
| CHEMBL99 | TRICHOSTATIN | 1.0 | 1 | 6.21 |
| CHEMBL1240974 | — | — | 1 | 6.19 |
| CHEMBL1242374 | PLADIENOLIDE F | — | 1 | 5.67 |
| CHEMBL374308 | LACTACYSTIN | — | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1242745 | PLADIENOLIDE B | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL1242564 | PLA D | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL1240972 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL1242467 | PLADIENOLIDE C | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1242284 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL269732 | TACROLIMUS ANHYDROUS | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL1242654 | PLADIENOLIDE E | IC50 | = | 58.9 | nM | 7.23 |
| CHEMBL1240973 | — | IC50 | = | 78.4 | nM | 7.11 |
| CHEMBL1242841 | PLADIENOLIDE A | IC50 | = | 307.7 | nM | 6.51 |
| CHEMBL99 | TRICHOSTATIN | IC50 | = | 611.2 | nM | 6.21 |
| CHEMBL1240974 | — | IC50 | = | 644.8 | nM | 6.19 |
| CHEMBL1242374 | PLADIENOLIDE F | IC50 | = | 2153.9 | nM | 5.67 |
| CHEMBL374308 | LACTACYSTIN | IC50 | = | 3481.0 | nM | 5.46 |