Assay Detail
Binding
CHEMBL4180673
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Displacement of 1,8-ANS from human N-terminal His-tagged RORgammat LBD (850 to 1635 residues) expressed in Escherichia coli by thermofluor 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 |
|---|---|---|---|
| Kd | 33 | 7.50 | 9.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4216372 | — | — | 1 | 9.57 |
| CHEMBL4204175 | — | — | 2 | 9.42 |
| CHEMBL4205065 | — | — | 1 | 9.30 |
| CHEMBL4217859 | — | — | 1 | 9.22 |
| CHEMBL4209944 | — | — | 1 | 8.96 |
| CHEMBL3964680 | — | — | 2 | 8.44 |
| CHEMBL3952077 | — | — | 1 | 8.30 |
| CHEMBL3968603 | — | — | 2 | 8.30 |
| CHEMBL4209998 | — | — | 1 | 8.28 |
| CHEMBL4218386 | — | — | 1 | 8.19 |
| CHEMBL3957588 | — | — | 2 | 8.04 |
| CHEMBL4094197 | — | — | 1 | 7.85 |
| CHEMBL3972220 | — | — | 2 | 7.70 |
| CHEMBL4213458 | — | — | 1 | 7.51 |
| CHEMBL4071285 | — | — | 3 | 7.50 |
| CHEMBL4214388 | — | — | 1 | 7.42 |
| CHEMBL4209983 | — | — | 2 | 7.16 |
| CHEMBL4205629 | — | — | 1 | 7.12 |
| CHEMBL4218239 | — | — | 1 | 6.96 |
| CHEMBL4207122 | — | — | 1 | 6.72 |
| CHEMBL4206508 | — | — | 1 | 6.55 |
| CHEMBL4211999 | — | — | 1 | 6.35 |
| CHEMBL4211066 | — | — | 1 | 6.02 |
| CHEMBL4208253 | — | — | 1 | 5.82 |
| CHEMBL4210499 | — | — | 1 | 4.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4216372 | — | Kd | = | 0.27 | nM | 9.57 |
| CHEMBL4204175 | — | Kd | = | 0.38 | nM | 9.42 |
| CHEMBL4205065 | — | Kd | = | 0.5 | nM | 9.30 |
| CHEMBL4217859 | — | Kd | = | 0.6 | nM | 9.22 |
| CHEMBL4209944 | — | Kd | = | 1.1 | nM | 8.96 |
| CHEMBL4204175 | — | Kd | = | 1.2 | nM | 8.92 |
| CHEMBL3964680 | — | Kd | = | 3.6 | nM | 8.44 |
| CHEMBL3952077 | — | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL3968603 | — | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL4209998 | — | Kd | = | 5.3 | nM | 8.28 |
| CHEMBL4218386 | — | Kd | = | 6.4 | nM | 8.19 |
| CHEMBL3957588 | — | Kd | = | 9.2 | nM | 8.04 |
| CHEMBL4094197 | — | Kd | = | 14.0 | nM | 7.85 |
| CHEMBL3972220 | — | Kd | = | 20.0 | nM | 7.70 |
| CHEMBL4213458 | — | Kd | = | 31.0 | nM | 7.51 |
| CHEMBL4071285 | — | Kd | = | 32.0 | nM | 7.50 |
| CHEMBL3972220 | — | Kd | = | 33.0 | nM | 7.48 |
| CHEMBL4214388 | — | Kd | = | 38.0 | nM | 7.42 |
| CHEMBL3968603 | — | Kd | = | 70.0 | nM | 7.16 |
| CHEMBL4209983 | — | Kd | = | 69.0 | nM | 7.16 |
| CHEMBL4205629 | — | Kd | = | 76.0 | nM | 7.12 |
| CHEMBL3964680 | — | Kd | = | 77.0 | nM | 7.11 |
| CHEMBL4209983 | — | Kd | = | 91.0 | nM | 7.04 |
| CHEMBL4218239 | — | Kd | = | 110.0 | nM | 6.96 |
| CHEMBL4071285 | — | Kd | = | 160.0 | nM | 6.80 |
| CHEMBL4207122 | — | Kd | = | 190.0 | nM | 6.72 |
| CHEMBL4206508 | — | Kd | = | 280.0 | nM | 6.55 |
| CHEMBL4211999 | — | Kd | = | 450.0 | nM | 6.35 |
| CHEMBL3957588 | — | Kd | = | 520.0 | nM | 6.28 |
| CHEMBL4211066 | — | Kd | = | 960.0 | nM | 6.02 |
| CHEMBL4208253 | — | Kd | = | 1500.0 | nM | 5.82 |
| CHEMBL4071285 | — | Kd | = | 5700.0 | nM | 5.24 |
| CHEMBL4210499 | — | Kd | = | 20000.0 | nM | 4.70 |