Assay Detail
Binding
CHEMBL4401912
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Transactivation of GAL4-fused mouse RARalpha-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 | 7.41 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL38 | TRETINOIN | 4.0 | 1 | 8.92 |
| CHEMBL4572914 | — | — | 1 | 8.40 |
| CHEMBL345298 | — | — | 1 | 8.04 |
| CHEMBL4449668 | — | — | 1 | 7.80 |
| CHEMBL4588745 | — | — | 1 | 7.75 |
| CHEMBL4437942 | — | — | 1 | 7.75 |
| CHEMBL4439399 | — | — | 1 | 7.72 |
| CHEMBL4459692 | — | — | 1 | 7.58 |
| CHEMBL4438880 | — | — | 1 | 7.52 |
| CHEMBL4442948 | — | — | 1 | 7.51 |
| CHEMBL4215742 | — | — | 1 | 7.34 |
| CHEMBL4439947 | — | — | 1 | 7.24 |
| CHEMBL4517145 | — | — | 1 | 7.22 |
| CHEMBL4531897 | — | — | 1 | 7.21 |
| CHEMBL198997 | — | — | 1 | 7.16 |
| CHEMBL4469143 | — | — | 1 | 7.05 |
| CHEMBL4562084 | — | — | 1 | 6.94 |
| CHEMBL4539676 | — | — | 1 | 6.62 |
| CHEMBL4590840 | — | — | 1 | 6.23 |
| CHEMBL4448702 | — | — | 1 | 6.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL38 | TRETINOIN | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4572914 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL345298 | — | EC50 | = | 9.2 | nM | 8.04 |
| CHEMBL4449668 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4588745 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4437942 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4439399 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4459692 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4438880 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4442948 | — | EC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4215742 | — | EC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4439947 | — | EC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4517145 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4531897 | — | EC50 | = | 61.0 | nM | 7.21 |
| CHEMBL198997 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4469143 | — | EC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4562084 | — | EC50 | = | 114.0 | nM | 6.94 |
| CHEMBL4539676 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4590840 | — | EC50 | = | 594.0 | nM | 6.23 |
| CHEMBL4448702 | — | EC50 | = | 600.0 | nM | 6.22 |