Assay Detail
Binding
CHEMBL4151885
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inverse agonist activity at biotinylated HN-Avi-MBP-TCS-human RORgammat (258 to 518 residues) assessed as inhibition of biotinylated SRC-1 peptide NCOA1 (677 to 700 residues) recruitment incubated with coactivator peptide 15 mins before enzyme addition and further incubated for 1 hr by HTRF-FRET assay
30
Total Activities
30
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 | 30 | 7.05 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4168454 | — | — | 1 | 7.68 |
| CHEMBL3105681 | — | — | 1 | 7.66 |
| CHEMBL3105692 | — | — | 1 | 7.64 |
| CHEMBL4160227 | — | — | 1 | 7.54 |
| CHEMBL4163215 | — | — | 1 | 7.52 |
| CHEMBL4166982 | — | — | 1 | 7.52 |
| CHEMBL4167096 | — | — | 1 | 7.52 |
| CHEMBL4173467 | — | — | 1 | 7.52 |
| CHEMBL4159395 | — | — | 1 | 7.52 |
| CHEMBL4159819 | — | — | 1 | 7.47 |
| CHEMBL4161696 | — | — | 1 | 7.40 |
| CHEMBL4173025 | — | — | 1 | 7.40 |
| CHEMBL4167788 | — | — | 1 | 7.30 |
| CHEMBL4169028 | — | — | 1 | 7.26 |
| CHEMBL4176513 | — | — | 1 | 7.22 |
| CHEMBL4168496 | — | — | 1 | 7.20 |
| CHEMBL4174976 | — | — | 1 | 7.17 |
| CHEMBL4163193 | — | — | 1 | 7.14 |
| CHEMBL4176887 | — | — | 1 | 7.12 |
| CHEMBL4170357 | — | — | 1 | 7.10 |
| CHEMBL4165905 | — | — | 1 | 7.05 |
| CHEMBL4162759 | — | — | 1 | 6.96 |
| CHEMBL4165121 | — | — | 1 | 6.92 |
| CHEMBL4161408 | — | — | 1 | 6.75 |
| CHEMBL4169629 | — | — | 1 | 6.36 |
| CHEMBL4171536 | — | — | 1 | 6.34 |
| CHEMBL4166203 | — | — | 1 | 6.16 |
| CHEMBL4170027 | — | — | 1 | 6.11 |
| CHEMBL4171845 | — | — | 1 | 5.49 |
| CHEMBL4170472 | — | — | 1 | 5.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4168454 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3105681 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3105692 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4160227 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4163215 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4166982 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4167096 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4173467 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4159395 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4159819 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4161696 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4173025 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4167788 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4169028 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4176513 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4168496 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4174976 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4163193 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4176887 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4170357 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4165905 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4162759 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4165121 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4161408 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4169629 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4171536 | — | IC50 | = | 452.0 | nM | 6.34 |
| CHEMBL4166203 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4170027 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL4171845 | — | IC50 | = | 3250.0 | nM | 5.49 |
| CHEMBL4170472 | — | IC50 | = | 3530.0 | nM | 5.45 |