Assay Detail
Binding
CHEMBL4820804
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inverse agonist activity at recombinant full-length human Gal4-fused RORgammat expressed in human Jurkat cells incubated for 18 hrs by steady-glo luciferase reporter gene assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Jurkat |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Tricyclic-Carbocyclic RORγt Inverse Agonists-Discovery of BMS-986313.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 29 | 8.08 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4848024 | — | — | 1 | 8.85 |
| CHEMBL4858617 | — | — | 1 | 8.72 |
| CHEMBL4862214 | — | — | 1 | 8.66 |
| CHEMBL4784900 | — | — | 1 | 8.60 |
| CHEMBL4852430 | — | — | 1 | 8.60 |
| CHEMBL4868491 | — | — | 1 | 8.51 |
| CHEMBL4761772 | — | — | 1 | 8.44 |
| CHEMBL4873930 | — | — | 1 | 8.43 |
| CHEMBL4877606 | — | — | 1 | 8.35 |
| CHEMBL4864029 | — | — | 1 | 8.27 |
| CHEMBL4870806 | — | — | 1 | 8.27 |
| CHEMBL4867702 | — | — | 1 | 8.17 |
| CHEMBL4873153 | — | — | 1 | 8.14 |
| CHEMBL4863937 | — | — | 1 | 8.13 |
| CHEMBL4859011 | — | — | 1 | 8.07 |
| CHEMBL4866347 | — | — | 1 | 8.07 |
| CHEMBL4859021 | — | — | 1 | 8.06 |
| CHEMBL4860008 | — | — | 1 | 8.04 |
| CHEMBL4878821 | — | — | 1 | 8.00 |
| CHEMBL4871326 | — | — | 1 | 7.92 |
| CHEMBL4860095 | — | — | 1 | 7.91 |
| CHEMBL4848053 | — | — | 1 | 7.82 |
| CHEMBL4861565 | — | — | 1 | 7.70 |
| CHEMBL4874499 | — | — | 1 | 7.62 |
| CHEMBL4863650 | — | — | 1 | 7.58 |
| CHEMBL4861441 | — | — | 1 | 7.52 |
| CHEMBL4850496 | — | — | 1 | 7.35 |
| CHEMBL4846596 | — | — | 1 | 7.32 |
| CHEMBL4861529 | — | — | 1 | 7.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4848024 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4858617 | — | EC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4862214 | — | EC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4784900 | — | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4852430 | — | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4868491 | — | EC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4761772 | — | EC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4873930 | — | EC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4877606 | — | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4864029 | — | EC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4870806 | — | EC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4867702 | — | EC50 | = | 6.7 | nM | 8.17 |
| CHEMBL4873153 | — | EC50 | = | 7.3 | nM | 8.14 |
| CHEMBL4863937 | — | EC50 | = | 7.4 | nM | 8.13 |
| CHEMBL4859011 | — | EC50 | = | 8.5 | nM | 8.07 |
| CHEMBL4866347 | — | EC50 | = | 8.6 | nM | 8.07 |
| CHEMBL4859021 | — | EC50 | = | 8.7 | nM | 8.06 |
| CHEMBL4860008 | — | EC50 | = | 9.1 | nM | 8.04 |
| CHEMBL4878821 | — | EC50 | = | 9.9 | nM | 8.00 |
| CHEMBL4871326 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4860095 | — | EC50 | = | 12.3 | nM | 7.91 |
| CHEMBL4848053 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4861565 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4874499 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4863650 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4861441 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4850496 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4846596 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4861529 | — | EC50 | = | 63.0 | nM | 7.20 |