Assay Detail
Binding
CHEMBL5032820
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Inhibition of RPE65 in bovine retinal pigment epithelium microsomes assessed as decrease of 11-cis-retinol using trans-retinol measured after 1 hr by normal phase HPLC analysis
21
Total Activities
18
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
Rational Alteration of Pharmacokinetics of Chiral Fluorinated and Deuterated Derivatives of Emixustat for Retinal Therapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.73 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5083918 | — | — | 1 | 7.30 |
| CHEMBL5091011 | — | — | 1 | 7.02 |
| CHEMBL5080647 | — | — | 1 | 6.99 |
| CHEMBL5094849 | — | — | 1 | 6.91 |
| CHEMBL5069771 | — | — | 2 | 6.88 |
| CHEMBL5081450 | — | — | 1 | 6.84 |
| CHEMBL5081640 | — | — | 1 | 6.77 |
| CHEMBL4781327 | — | — | 1 | 6.76 |
| CHEMBL5094949 | — | — | 1 | 6.75 |
| CHEMBL5077356 | — | — | 2 | 6.74 |
| CHEMBL5082794 | — | — | 1 | 6.72 |
| CHEMBL5084662 | — | — | 1 | 6.70 |
| CHEMBL5075304 | — | — | 1 | 6.57 |
| CHEMBL5083435 | — | — | 2 | 6.56 |
| CHEMBL5092414 | — | — | 1 | 6.55 |
| CHEMBL5086566 | — | — | 1 | 6.54 |
| CHEMBL4757869 | — | — | 1 | 6.49 |
| CHEMBL5076106 | — | — | 1 | 6.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5083918 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5091011 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL5080647 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL5094849 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL5069771 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL5081450 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL5069771 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL5081640 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL4781327 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL5094949 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL5077356 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL5082794 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5084662 | — | IC50 | = | 201.0 | nM | 6.70 |
| CHEMBL5075304 | — | IC50 | = | 269.0 | nM | 6.57 |
| CHEMBL5083435 | — | IC50 | = | 274.0 | nM | 6.56 |
| CHEMBL5092414 | — | IC50 | = | 284.0 | nM | 6.55 |
| CHEMBL5083435 | — | IC50 | = | 287.0 | nM | 6.54 |
| CHEMBL5086566 | — | IC50 | = | 292.0 | nM | 6.54 |
| CHEMBL5077356 | — | IC50 | = | 295.0 | nM | 6.53 |
| CHEMBL4757869 | — | IC50 | = | 323.0 | nM | 6.49 |
| CHEMBL5076106 | — | IC50 | = | 358.0 | nM | 6.45 |