Assay Detail
Binding
CHEMBL4623385
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Binding affinity to recombinant human RORgammat transfected in human HEK293T cells incubated for 24 hrs by dual-glo luciferase reporter gene assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK-293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and optimization of new oxadiazole substituted thiazole RORγt inverse agonists through a bioisosteric amide replacement approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 8.04 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4635823 | — | — | 1 | 10.00 |
| CHEMBL4647899 | — | — | 1 | 8.80 |
| CHEMBL4128926 | — | — | 1 | 8.70 |
| CHEMBL4129202 | — | — | 1 | 8.59 |
| CHEMBL4637144 | — | — | 1 | 8.49 |
| CHEMBL4642631 | — | — | 1 | 8.44 |
| CHEMBL4632527 | — | — | 1 | 8.44 |
| CHEMBL4647734 | — | — | 1 | 8.37 |
| CHEMBL4642450 | — | — | 1 | 8.22 |
| CHEMBL4649094 | — | — | 1 | 8.10 |
| CHEMBL4633899 | — | — | 1 | 8.10 |
| CHEMBL4637003 | — | — | 1 | 8.05 |
| CHEMBL4645288 | — | — | 1 | 7.96 |
| CHEMBL4641138 | — | — | 1 | 7.89 |
| CHEMBL4648607 | — | — | 1 | 7.87 |
| CHEMBL4642733 | — | — | 1 | 7.85 |
| CHEMBL4649210 | — | — | 1 | 7.82 |
| CHEMBL4632490 | — | — | 1 | 7.80 |
| CHEMBL4649863 | — | — | 1 | 7.80 |
| CHEMBL4648849 | — | — | 1 | 7.68 |
| CHEMBL4642674 | — | — | 1 | 7.66 |
| CHEMBL4633325 | — | — | 1 | 7.62 |
| CHEMBL4641039 | — | — | 1 | 7.60 |
| CHEMBL4634072 | — | — | 1 | 7.57 |
| CHEMBL4634974 | — | — | 1 | 7.57 |
| CHEMBL4649427 | — | — | 1 | 7.48 |
| CHEMBL4644116 | — | — | 1 | 7.35 |
| CHEMBL4645942 | — | — | 1 | 7.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4635823 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4647899 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4128926 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4129202 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4637144 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4642631 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4632527 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4647734 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4642450 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4649094 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4633899 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4637003 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4645288 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4641138 | — | IC50 | = | 12.8 | nM | 7.89 |
| CHEMBL4648607 | — | IC50 | = | 13.5 | nM | 7.87 |
| CHEMBL4642733 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4649210 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4632490 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4649863 | — | IC50 | = | 15.7 | nM | 7.80 |
| CHEMBL4648849 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4642674 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4633325 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4641039 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4634072 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4634974 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4649427 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4644116 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4645942 | — | IC50 | = | 47.0 | nM | 7.33 |