Assay Detail
Binding
CHEMBL645946
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Concentration required to inhibit activator protein-1(AP-1) mediated transcriptional activation in human Jurkat T-cells
25
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Jurkat |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Inhibitors of NF-kappaB and AP-1 gene expression: SAR studies on the pyrimidine portion of 2-chloro-4-trifluoromethylpyrimidine-5-[N-(3', 5'-bis(trifluoromethyl)phenyl)carboxamide].
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.30 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL132495 | — | — | 1 | 7.70 |
| CHEMBL336546 | — | — | 1 | 7.30 |
| CHEMBL131006 | — | — | 1 | 7.00 |
| CHEMBL340779 | — | — | 1 | 6.70 |
| CHEMBL339462 | — | — | 1 | 6.52 |
| CHEMBL337656 | — | — | 1 | 6.52 |
| CHEMBL423150 | — | — | 1 | 6.40 |
| CHEMBL262514 | — | — | 1 | 6.30 |
| CHEMBL421280 | — | — | 1 | 6.22 |
| CHEMBL338934 | — | — | 1 | 5.77 |
| CHEMBL340410 | — | — | 1 | 5.40 |
| CHEMBL128599 | — | — | 1 | 5.10 |
| CHEMBL128708 | — | — | 1 | 5.00 |
| CHEMBL131007 | — | — | 1 | - |
| CHEMBL128808 | — | — | 1 | - |
| CHEMBL132457 | — | — | 1 | - |
| CHEMBL340165 | — | — | 1 | - |
| CHEMBL128314 | — | — | 1 | - |
| CHEMBL131293 | — | — | 1 | - |
| CHEMBL128053 | — | — | 1 | - |
| CHEMBL128426 | — | — | 1 | - |
| CHEMBL441830 | — | — | 2 | - |
| CHEMBL131246 | — | — | 1 | - |
| CHEMBL128598 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL132495 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL336546 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL131006 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL340779 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL339462 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL337656 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL423150 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL262514 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL421280 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL338934 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL340410 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL128599 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL128708 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL131007 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL441830 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL128808 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL340165 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL132457 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL128314 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL131293 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL128053 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL128426 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL441830 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL131246 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL128598 | — | IC50 | > | 10000.0 | nM | - |