Assay Detail
Binding
CHEMBL4401915
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Transactivation of GAL4-fused mouse RARgamma-LBD expressed in COS-7 cells after 24 hrs by bright-Glo reagent based assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and lead optimisation of a potent, selective and orally bioavailable RARβ agonist for the potential treatment of nerve injury.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 20 | 7.79 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL38 | TRETINOIN | 4.0 | 1 | 9.22 |
| CHEMBL4572914 | — | — | 1 | 8.55 |
| CHEMBL4442948 | — | — | 1 | 8.27 |
| CHEMBL4531897 | — | — | 1 | 8.26 |
| CHEMBL198997 | — | — | 1 | 8.24 |
| CHEMBL4469143 | — | — | 1 | 8.19 |
| CHEMBL4449668 | — | — | 1 | 8.14 |
| CHEMBL4439399 | — | — | 1 | 8.12 |
| CHEMBL4438880 | — | — | 1 | 8.05 |
| CHEMBL4562084 | — | — | 1 | 8.00 |
| CHEMBL345298 | — | — | 1 | 7.96 |
| CHEMBL4588745 | — | — | 1 | 7.92 |
| CHEMBL4459692 | — | — | 1 | 7.89 |
| CHEMBL4448702 | — | — | 1 | 7.89 |
| CHEMBL4517145 | — | — | 1 | 7.35 |
| CHEMBL4439947 | — | — | 1 | 6.82 |
| CHEMBL4539676 | — | — | 1 | 6.80 |
| CHEMBL4215742 | — | — | 1 | 4.52 |
| CHEMBL4437942 | — | — | 1 | - |
| CHEMBL4590840 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL38 | TRETINOIN | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4572914 | — | EC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4442948 | — | EC50 | = | 5.4 | nM | 8.27 |
| CHEMBL4531897 | — | EC50 | = | 5.5 | nM | 8.26 |
| CHEMBL198997 | — | EC50 | = | 5.8 | nM | 8.24 |
| CHEMBL4469143 | — | EC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4449668 | — | EC50 | = | 7.3 | nM | 8.14 |
| CHEMBL4439399 | — | EC50 | = | 7.6 | nM | 8.12 |
| CHEMBL4438880 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4562084 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL345298 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4588745 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4459692 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4448702 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4517145 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4439947 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4539676 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4215742 | — | EC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL4437942 | — | EC50 | = | 0.0043 | nM | - |
| CHEMBL4590840 | — | EC50 | - | — | - |