Assay Detail
Binding
CHEMBL3762006
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human OAT3 expressed in HEK cells assessed as reduction of [3H]-estrone sulfate uptake by radioactivity counting analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of N-(4-Fluoro-3-methoxybenzyl)-6-(2-(((2S,5R)-5-(hydroxymethyl)-1,4-dioxan-2-yl)methyl)-2H-tetrazol-5-yl)-2-methylpyrimidine-4-carboxamide. A Highly Selective and Orally Bioavailable Matrix Metalloproteinase-13 Inhibitor for the Potential Treatment of Osteoarthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 4.73 | 5.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL603656 | — | — | 1 | 5.22 |
| CHEMBL496942 | — | — | 1 | 4.75 |
| CHEMBL270050 | — | — | 1 | 4.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL603656 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL496942 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL270050 | — | IC50 | = | 59000.0 | nM | 4.23 |