Assay Detail
Functional
CHEMBL705830
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Inhibition of AP-1 and NF-kB mediated transcriptional activation in Jurkat T-cells
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Jurkat |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
The design and synthesis of novel orally active inhibitors of AP-1 and NF-kappaB mediated transcriptional activation. SAR of in vitro and in vivo studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.21 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL337665 | — | — | 1 | 8.52 |
| CHEMBL129857 | AS-602868 | 1.0 | 1 | 8.10 |
| CHEMBL133412 | — | — | 1 | 8.00 |
| CHEMBL133622 | — | — | 1 | 7.70 |
| CHEMBL130406 | — | — | 1 | 7.70 |
| CHEMBL337640 | — | — | 1 | 7.70 |
| CHEMBL131953 | — | — | 1 | 7.70 |
| CHEMBL130204 | — | — | 1 | 7.52 |
| CHEMBL335904 | — | — | 1 | 7.40 |
| CHEMBL336770 | — | — | 1 | 7.40 |
| CHEMBL131132 | — | — | 1 | 7.30 |
| CHEMBL130752 | — | — | 1 | 7.30 |
| CHEMBL133379 | — | — | 1 | 7.30 |
| CHEMBL130837 | — | — | 1 | 7.22 |
| CHEMBL134245 | — | — | 1 | 7.10 |
| CHEMBL130007 | — | — | 1 | 7.00 |
| CHEMBL335612 | — | — | 1 | 7.00 |
| CHEMBL133245 | — | — | 1 | 7.00 |
| CHEMBL133631 | — | — | 1 | 6.70 |
| CHEMBL129940 | — | — | 1 | 6.70 |
| CHEMBL336408 | — | — | 1 | 6.40 |
| CHEMBL336177 | — | — | 1 | 6.00 |
| CHEMBL130057 | — | — | 1 | 5.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL337665 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL129857 | AS-602868 | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL133412 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL133622 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL130406 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL337640 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL131953 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL130204 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL335904 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL336770 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL131132 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL130752 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL133379 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL130837 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL134245 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL130007 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL335612 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL133245 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL133631 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL129940 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL336408 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL336177 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL130057 | — | IC50 | = | 9000.0 | nM | 5.05 |