Assay Detail
Binding
CHEMBL3106085
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Inhibition of RORgammat receptor ligand binding domain in mouse spleen CD4+ T cells assessed as inhibition of IL-17 production after 3 days by ELISA
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Tissue | Spleen |
| Cell Type | T-cell |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of novel N-(5-(arylcarbonyl)thiazol-2-yl)amides and N-(5-(arylcarbonyl)thiophen-2-yl)amides as potent RORγt inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.07 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3105690 | — | — | 1 | 8.00 |
| CHEMBL3105670 | — | — | 1 | 8.00 |
| CHEMBL3105672 | — | — | 1 | 7.90 |
| CHEMBL3105671 | — | — | 1 | 7.80 |
| CHEMBL3105669 | — | — | 1 | 7.60 |
| CHEMBL3105692 | — | — | 1 | 7.60 |
| CHEMBL3105691 | — | — | 1 | 7.60 |
| CHEMBL3105686 | — | — | 1 | 7.30 |
| CHEMBL3105676 | — | — | 1 | 6.90 |
| CHEMBL3105678 | — | — | 1 | 6.80 |
| CHEMBL3105685 | — | — | 1 | 6.70 |
| CHEMBL3105681 | — | — | 1 | 6.70 |
| CHEMBL3105682 | — | — | 1 | 6.60 |
| CHEMBL3105674 | — | — | 1 | 6.50 |
| CHEMBL3105684 | — | — | 1 | 6.50 |
| CHEMBL3105675 | — | — | 1 | 6.40 |
| CHEMBL3105683 | — | — | 1 | 6.20 |
| CHEMBL3105677 | — | — | 1 | 6.10 |
| CHEMBL3105679 | — | — | 1 | - |
| CHEMBL3105680 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3105690 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3105670 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3105672 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL3105671 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL3105669 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL3105692 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL3105691 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL3105686 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL3105676 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3105678 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL3105685 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL3105681 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL3105682 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL3105674 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL3105684 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL3105675 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL3105683 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL3105677 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL3105679 | — | IC50 | > | 7943.28 | nM | - |
| CHEMBL3105680 | — | IC50 | > | 10000.0 | nM | - |