Assay Detail
Binding
CHEMBL5158491
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at AhR in human recombinant HepG2-Lucia AhR cell incubated for 24 hrs by luciferase reporter gene assay
39
Total Activities
39
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
Identification of triazolopyridine derivatives as a new class of AhR agonists and evaluation of anti-psoriasis effect in a mouse model.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 39 | 7.01 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5203882 | — | — | 1 | 10.52 |
| CHEMBL5190861 | — | — | 1 | 9.57 |
| CHEMBL5021347 | — | — | 1 | 9.47 |
| CHEMBL5194336 | — | — | 1 | 9.36 |
| CHEMBL5181725 | — | — | 1 | 9.08 |
| CHEMBL5199691 | — | — | 1 | 8.02 |
| CHEMBL5198934 | — | — | 1 | 7.64 |
| CHEMBL259571 | TAPINAROF | 4.0 | 1 | 7.56 |
| CHEMBL5195426 | — | — | 1 | 7.21 |
| CHEMBL5183442 | — | — | 1 | 7.11 |
| CHEMBL5207451 | — | — | 1 | 7.08 |
| CHEMBL5173018 | — | — | 1 | 6.81 |
| CHEMBL5203209 | — | — | 1 | 6.76 |
| CHEMBL5194855 | — | — | 1 | 6.69 |
| CHEMBL5195658 | — | — | 1 | 6.57 |
| CHEMBL5208085 | — | — | 1 | 6.43 |
| CHEMBL5197557 | — | — | 1 | 6.20 |
| CHEMBL5207284 | — | — | 1 | 6.20 |
| CHEMBL5196574 | — | — | 1 | 6.18 |
| CHEMBL5172120 | — | — | 1 | 6.12 |
| CHEMBL5206725 | — | — | 1 | 6.08 |
| CHEMBL5190444 | — | — | 1 | 5.96 |
| CHEMBL5183167 | — | — | 1 | 5.93 |
| CHEMBL5193339 | — | — | 1 | 5.72 |
| CHEMBL5196709 | — | — | 1 | 5.61 |
| CHEMBL5172858 | — | — | 1 | 5.60 |
| CHEMBL5181229 | — | — | 1 | 5.48 |
| CHEMBL5174957 | — | — | 1 | 5.33 |
| CHEMBL5189144 | — | — | 1 | - |
| CHEMBL5170959 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5203882 | — | EC50 | = | 0.03 | nM | 10.52 |
| CHEMBL5190861 | — | EC50 | = | 0.27 | nM | 9.57 |
| CHEMBL5021347 | — | EC50 | = | 0.34 | nM | 9.47 |
| CHEMBL5194336 | — | EC50 | = | 0.44 | nM | 9.36 |
| CHEMBL5181725 | — | EC50 | = | 0.83 | nM | 9.08 |
| CHEMBL5199691 | — | EC50 | = | 9.6 | nM | 8.02 |
| CHEMBL5198934 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL259571 | TAPINAROF | EC50 | = | 27.34 | nM | 7.56 |
| CHEMBL5195426 | — | EC50 | = | 62.0 | nM | 7.21 |
| CHEMBL5183442 | — | EC50 | = | 77.0 | nM | 7.11 |
| CHEMBL5207451 | — | EC50 | = | 83.0 | nM | 7.08 |
| CHEMBL5173018 | — | EC50 | = | 156.0 | nM | 6.81 |
| CHEMBL5203209 | — | EC50 | = | 172.0 | nM | 6.76 |
| CHEMBL5194855 | — | EC50 | = | 205.0 | nM | 6.69 |
| CHEMBL5195658 | — | EC50 | = | 271.0 | nM | 6.57 |
| CHEMBL5208085 | — | EC50 | = | 374.0 | nM | 6.43 |
| CHEMBL5197557 | — | EC50 | = | 625.0 | nM | 6.20 |
| CHEMBL5207284 | — | EC50 | = | 625.0 | nM | 6.20 |
| CHEMBL5196574 | — | EC50 | = | 658.0 | nM | 6.18 |
| CHEMBL5172120 | — | EC50 | = | 759.0 | nM | 6.12 |
| CHEMBL5206725 | — | EC50 | = | 842.0 | nM | 6.08 |
| CHEMBL5190444 | — | EC50 | = | 1093.0 | nM | 5.96 |
| CHEMBL5183167 | — | EC50 | = | 1185.0 | nM | 5.93 |
| CHEMBL5193339 | — | EC50 | = | 1895.0 | nM | 5.72 |
| CHEMBL5196709 | — | EC50 | = | 2430.0 | nM | 5.61 |
| CHEMBL5172858 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL5181229 | — | EC50 | = | 3330.0 | nM | 5.48 |
| CHEMBL5174957 | — | EC50 | = | 4660.0 | nM | 5.33 |
| CHEMBL5183426 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5197056 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5194508 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5171041 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5189053 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5207468 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5200189 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5189377 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5173875 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5170959 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5189144 | — | EC50 | > | 10000.0 | nM | - |