Assay Detail
Binding
CHEMBL4180674
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Inverse agonist activity at GAL4 DBD-fused wild type human RORgammat LBD (850 to 1635 residues) expressed in HEK293T cells assessed as inhibition of transcriptional activity after 24 hrs by dual-glo luciferase reporter gene assay
33
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
6-Substituted quinolines as RORγt inverse agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 6.92 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4204175 | — | — | 2 | 8.28 |
| CHEMBL4205065 | — | — | 1 | 8.26 |
| CHEMBL3952077 | — | — | 1 | 8.18 |
| CHEMBL4217859 | — | — | 1 | 7.89 |
| CHEMBL4209998 | — | — | 1 | 7.68 |
| CHEMBL3964680 | — | — | 2 | 7.62 |
| CHEMBL3972220 | — | — | 2 | 7.34 |
| CHEMBL4094197 | — | — | 1 | 7.30 |
| CHEMBL3957588 | — | — | 2 | 7.14 |
| CHEMBL4218386 | — | — | 1 | 7.09 |
| CHEMBL3968603 | — | — | 2 | 7.05 |
| CHEMBL4209944 | — | — | 1 | 7.00 |
| CHEMBL4205629 | — | — | 1 | 6.89 |
| CHEMBL4214388 | — | — | 1 | 6.85 |
| CHEMBL4213458 | — | — | 1 | 6.75 |
| CHEMBL4216372 | — | — | 1 | 6.70 |
| CHEMBL4218239 | — | — | 1 | 6.68 |
| CHEMBL4071285 | — | — | 3 | 6.66 |
| CHEMBL4209983 | — | — | 2 | 6.57 |
| CHEMBL4207122 | — | — | 1 | 6.22 |
| CHEMBL4206508 | — | — | 1 | 6.20 |
| CHEMBL4211999 | — | — | 1 | 6.09 |
| CHEMBL4211066 | — | — | 1 | 6.00 |
| CHEMBL4208253 | — | — | 1 | 5.68 |
| CHEMBL4210499 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4204175 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4205065 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL3952077 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL4217859 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4204175 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4209998 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3964680 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3972220 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4094197 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3972220 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3957588 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL4218386 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL3968603 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4209944 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4205629 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3964680 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4214388 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3968603 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4213458 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4216372 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4218239 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4071285 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4071285 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4209983 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4209983 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4207122 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4206508 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL3957588 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL4211999 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4211066 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4208253 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4071285 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL4210499 | — | IC50 | > | 6000.0 | nM | - |