Assay Detail
Binding
CHEMBL4151884
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-2-(4-(ethylsulfonyl)phenyl)-N-(4-(2-(methoxymethyl)phenyl)thiophen-2-yl)acetamide from purified N-(HN)6-GST-TCS-human RORgammat (258 to 518 residues) incubated for 16 hrs by scintillation proximity assay
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Potent and Orally Bioavailable Inverse Agonists of RORγt Resulting from Structure-Based Design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 7.41 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4167096 | — | — | 1 | 8.70 |
| CHEMBL3105692 | — | — | 1 | 8.70 |
| CHEMBL4159819 | — | — | 1 | 8.52 |
| CHEMBL4176887 | — | — | 1 | 8.22 |
| CHEMBL4173908 | — | — | 1 | 8.15 |
| CHEMBL4163193 | — | — | 1 | 8.15 |
| CHEMBL4163215 | — | — | 1 | 8.15 |
| CHEMBL3105681 | — | — | 1 | 8.05 |
| CHEMBL4168496 | — | — | 1 | 8.05 |
| CHEMBL4166982 | — | — | 1 | 8.00 |
| CHEMBL4160227 | — | — | 1 | 7.96 |
| CHEMBL4174976 | — | — | 1 | 7.85 |
| CHEMBL4168454 | — | — | 1 | 7.85 |
| CHEMBL4175680 | — | — | 1 | 7.77 |
| CHEMBL4167788 | — | — | 1 | 7.75 |
| CHEMBL4159082 | — | — | 1 | 7.72 |
| CHEMBL4176822 | — | — | 1 | 7.70 |
| CHEMBL4173467 | — | — | 1 | 7.70 |
| CHEMBL4159395 | — | — | 1 | 7.70 |
| CHEMBL4165060 | — | — | 1 | 7.54 |
| CHEMBL4161696 | — | — | 1 | 7.52 |
| CHEMBL4170500 | — | — | 1 | 7.48 |
| CHEMBL4167413 | — | — | 1 | 7.34 |
| CHEMBL4165905 | — | — | 1 | 7.30 |
| CHEMBL4176513 | — | — | 1 | 7.30 |
| CHEMBL4175289 | — | — | 1 | 7.23 |
| CHEMBL4169028 | — | — | 1 | 7.18 |
| CHEMBL4173025 | — | — | 1 | 7.16 |
| CHEMBL4171536 | — | — | 1 | 7.12 |
| CHEMBL4174263 | — | — | 1 | 7.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4167096 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3105692 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4159819 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4176887 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4173908 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4163193 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4163215 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3105681 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4168496 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4166982 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4160227 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4174976 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4168454 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4175680 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4167788 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4159082 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4176822 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4173467 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4159395 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4165060 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4161696 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4170500 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4167413 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4165905 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4176513 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4175289 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4169028 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4173025 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4171536 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4174263 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL4161408 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4170357 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4170472 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4165121 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4162759 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4170027 | — | IC50 | = | 1160.0 | nM | 5.94 |
| CHEMBL4169629 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL4166203 | — | IC50 | = | 1850.0 | nM | 5.73 |
| CHEMBL4171845 | — | IC50 | = | 3250.0 | nM | 5.49 |