Assay Detail
Binding
CHEMBL4623384
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Binding affinity to RORgammat (unknown origin) assessed as dissociation constant by thermal shift binding assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 |
|---|---|---|---|
| Kd | 29 | 8.93 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4642631 | — | — | 1 | 10.52 |
| CHEMBL4637144 | — | — | 1 | 10.40 |
| CHEMBL4647899 | — | — | 1 | 10.30 |
| CHEMBL4633899 | — | — | 1 | 10.15 |
| CHEMBL4128926 | — | — | 1 | 9.92 |
| CHEMBL4641138 | — | — | 1 | 9.57 |
| CHEMBL4642674 | — | — | 1 | 9.52 |
| CHEMBL4642450 | — | — | 1 | 9.46 |
| CHEMBL4647734 | — | — | 1 | 9.44 |
| CHEMBL4632527 | — | — | 1 | 9.41 |
| CHEMBL4645288 | — | — | 1 | 9.30 |
| CHEMBL4649427 | — | — | 1 | 9.15 |
| CHEMBL4648607 | — | — | 1 | 9.09 |
| CHEMBL4129202 | — | — | 1 | 8.96 |
| CHEMBL4633325 | — | — | 1 | 8.82 |
| CHEMBL4649210 | — | — | 1 | 8.82 |
| CHEMBL4636398 | — | — | 1 | 8.77 |
| CHEMBL4637003 | — | — | 1 | 8.70 |
| CHEMBL4641039 | — | — | 1 | 8.64 |
| CHEMBL4649094 | — | — | 1 | 8.57 |
| CHEMBL4642733 | — | — | 1 | 8.49 |
| CHEMBL4634974 | — | — | 1 | 8.41 |
| CHEMBL4634072 | — | — | 1 | 8.37 |
| CHEMBL4648849 | — | — | 1 | 8.30 |
| CHEMBL4649863 | — | — | 1 | 8.19 |
| CHEMBL4645942 | — | — | 1 | 8.06 |
| CHEMBL4644116 | — | — | 1 | 7.96 |
| CHEMBL4632490 | — | — | 1 | 4.85 |
| CHEMBL4635823 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4642631 | — | Kd | = | 0.03 | nM | 10.52 |
| CHEMBL4637144 | — | Kd | = | 0.04 | nM | 10.40 |
| CHEMBL4647899 | — | Kd | = | 0.05 | nM | 10.30 |
| CHEMBL4633899 | — | Kd | = | 0.07 | nM | 10.15 |
| CHEMBL4128926 | — | Kd | = | 0.12 | nM | 9.92 |
| CHEMBL4641138 | — | Kd | = | 0.27 | nM | 9.57 |
| CHEMBL4642674 | — | Kd | = | 0.3 | nM | 9.52 |
| CHEMBL4642450 | — | Kd | = | 0.35 | nM | 9.46 |
| CHEMBL4647734 | — | Kd | = | 0.36 | nM | 9.44 |
| CHEMBL4632527 | — | Kd | = | 0.39 | nM | 9.41 |
| CHEMBL4645288 | — | Kd | = | 0.5 | nM | 9.30 |
| CHEMBL4649427 | — | Kd | = | 0.7 | nM | 9.15 |
| CHEMBL4648607 | — | Kd | = | 0.82 | nM | 9.09 |
| CHEMBL4129202 | — | Kd | = | 1.1 | nM | 8.96 |
| CHEMBL4633325 | — | Kd | = | 1.5 | nM | 8.82 |
| CHEMBL4649210 | — | Kd | = | 1.5 | nM | 8.82 |
| CHEMBL4636398 | — | Kd | = | 1.7 | nM | 8.77 |
| CHEMBL4637003 | — | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL4641039 | — | Kd | = | 2.3 | nM | 8.64 |
| CHEMBL4649094 | — | Kd | = | 2.7 | nM | 8.57 |
| CHEMBL4642733 | — | Kd | = | 3.2 | nM | 8.49 |
| CHEMBL4634974 | — | Kd | = | 3.9 | nM | 8.41 |
| CHEMBL4634072 | — | Kd | = | 4.3 | nM | 8.37 |
| CHEMBL4648849 | — | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL4649863 | — | Kd | = | 6.5 | nM | 8.19 |
| CHEMBL4645942 | — | Kd | = | 8.7 | nM | 8.06 |
| CHEMBL4644116 | — | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL4632490 | — | Kd | = | 14169.0 | nM | 4.85 |
| CHEMBL4635823 | — | Kd | = | 0.003 | nM | - |