Assay Detail
Binding
CHEMBL5365762
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Agonist activity at AHR in human HepG2-Lucia AhR cells stably transfected with DRE by luciferase reporter assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HepG2-Lucia AhR |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of 5-((1H-indazol-3-yl) methylene)-2-thioxoimidazolidin-4-one derivatives as a new class of AHR agonists with anti-psoriasis activity in a mouse model.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 35 | 6.24 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5410096 | — | — | 1 | 7.82 |
| CHEMBL259571 | TAPINAROF | 4.0 | 1 | 7.57 |
| CHEMBL5418753 | — | — | 1 | 7.46 |
| CHEMBL5419477 | — | — | 1 | 7.31 |
| CHEMBL5406192 | — | — | 1 | 7.28 |
| CHEMBL5439352 | — | — | 1 | 6.84 |
| CHEMBL5434388 | — | — | 1 | 6.79 |
| CHEMBL5416301 | — | — | 1 | 6.66 |
| CHEMBL5399322 | — | — | 1 | 6.28 |
| CHEMBL5419189 | — | — | 1 | 6.21 |
| CHEMBL5426272 | — | — | 1 | 6.07 |
| CHEMBL5435523 | — | — | 1 | 5.75 |
| CHEMBL5429807 | — | — | 1 | 5.75 |
| CHEMBL5413861 | — | — | 1 | 5.60 |
| CHEMBL5434232 | — | — | 1 | 5.56 |
| CHEMBL5411787 | — | — | 1 | 5.55 |
| CHEMBL5410987 | — | — | 1 | 5.50 |
| CHEMBL5398518 | — | — | 1 | 5.47 |
| CHEMBL1624678 | — | — | 1 | 5.33 |
| CHEMBL5419047 | — | — | 1 | 5.23 |
| CHEMBL5400187 | — | — | 1 | 5.00 |
| CHEMBL5431457 | — | — | 1 | - |
| CHEMBL5429469 | — | — | 1 | - |
| CHEMBL5396882 | — | — | 1 | - |
| CHEMBL5398462 | — | — | 1 | - |
| CHEMBL5420784 | — | — | 1 | - |
| CHEMBL195008 | NECROSTATIN | — | 1 | - |
| CHEMBL5420973 | — | — | 1 | - |
| CHEMBL5393776 | — | — | 1 | - |
| CHEMBL38739 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5410096 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL259571 | TAPINAROF | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5418753 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5419477 | — | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5406192 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL5439352 | — | EC50 | = | 143.0 | nM | 6.84 |
| CHEMBL5434388 | — | EC50 | = | 163.0 | nM | 6.79 |
| CHEMBL5416301 | — | EC50 | = | 219.0 | nM | 6.66 |
| CHEMBL5399322 | — | EC50 | = | 528.0 | nM | 6.28 |
| CHEMBL5419189 | — | EC50 | = | 613.0 | nM | 6.21 |
| CHEMBL5426272 | — | EC50 | = | 858.0 | nM | 6.07 |
| CHEMBL5435523 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL5429807 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL5413861 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL5434232 | — | EC50 | = | 2770.0 | nM | 5.56 |
| CHEMBL5411787 | — | EC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL5410987 | — | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL5398518 | — | EC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL1624678 | — | EC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL5419047 | — | EC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL5400187 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL5430036 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5418142 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5403712 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5418120 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL541474 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL38739 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5393776 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5420973 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL195008 | NECROSTATIN | EC50 | > | 10000.0 | nM | - |
| CHEMBL5420784 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5398462 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5396882 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5429469 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5431457 | — | EC50 | > | 10000.0 | nM | - |