Assay Detail
Binding
CHEMBL4669201
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of RPE65 in bovine RPE microsomes assessed as reduction in 11-cis-retinol production using all-trans-retinol as substrate pre-incubated with enzyme for 5 mins followed by further incubation with all-trans-retinol for 1 hr by normal phase HPLC analysis
4
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Tissue | Retina |
| Subcellular | Microsome |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of chiral fluorinated alkyl derivatives of emixustat as drug candidates for the treatment of retinal degenerative diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 6.69 | 6.78 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4795212 | — | — | 2 | 6.78 |
| CHEMBL4781327 | — | — | 1 | 6.76 |
| CHEMBL4757869 | — | — | 1 | 6.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4795212 | — | EC50 | = | 165.6 | nM | 6.78 |
| CHEMBL4781327 | — | EC50 | = | 172.4 | nM | 6.76 |
| CHEMBL4795212 | — | EC50 | = | 196.5 | nM | 6.71 |
| CHEMBL4757869 | — | EC50 | = | 323.3 | nM | 6.49 |