Assay Detail
Binding
CHEMBL4151887
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Inverse agonist activity at RORgammat in human TH17 cells assessed as inhibition of IL17 release incubated for 4 days by HTRF assay
25
Total Activities
25
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 | 25 | 7.06 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3105692 | — | — | 1 | 8.22 |
| CHEMBL4159819 | — | — | 1 | 7.96 |
| CHEMBL4170472 | — | — | 1 | 7.64 |
| CHEMBL4163215 | — | — | 1 | 7.60 |
| CHEMBL4160227 | — | — | 1 | 7.60 |
| CHEMBL4176887 | — | — | 1 | 7.50 |
| CHEMBL4168454 | — | — | 1 | 7.46 |
| CHEMBL4163193 | — | — | 1 | 7.31 |
| CHEMBL4168496 | — | — | 1 | 7.24 |
| CHEMBL4167096 | — | — | 1 | 7.19 |
| CHEMBL4166982 | — | — | 1 | 7.00 |
| CHEMBL4167788 | — | — | 1 | 7.00 |
| CHEMBL4170500 | — | — | 1 | 6.84 |
| CHEMBL3105681 | — | — | 1 | 6.75 |
| CHEMBL4174263 | — | — | 1 | 6.72 |
| CHEMBL4169028 | — | — | 1 | 6.19 |
| CHEMBL4159395 | — | — | 1 | 6.16 |
| CHEMBL4174976 | — | — | 1 | 6.00 |
| CHEMBL4171536 | — | — | 1 | 5.77 |
| CHEMBL4175680 | — | — | 1 | - |
| CHEMBL4161408 | — | — | 1 | - |
| CHEMBL4162759 | — | — | 1 | - |
| CHEMBL4173467 | — | — | 1 | - |
| CHEMBL4173025 | — | — | 1 | - |
| CHEMBL4161696 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3105692 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4159819 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4170472 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4163215 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4160227 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4176887 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4168454 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4163193 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4168496 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4167096 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4166982 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4167788 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4170500 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL3105681 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4174263 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4169028 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL4159395 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4174976 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL4171536 | — | IC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL4175680 | — | IC50 | > | 3300.0 | nM | - |
| CHEMBL4161408 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4162759 | — | IC50 | - | — | - | |
| CHEMBL4173467 | — | IC50 | > | 3300.0 | nM | - |
| CHEMBL4173025 | — | IC50 | > | 3300.0 | nM | - |
| CHEMBL4161696 | — | IC50 | > | 3300.0 | nM | - |