Assay Detail
Binding
CHEMBL699706
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Concentration required to inhibit the maximum [14C]Gly-Sar uptake by human Intestinal peptide transporter PepT1 in Caco-2 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Caco-2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Phe-Gly dipeptidomimetics designed for the di-/tripeptide transporters PEPT1 and PEPT2: synthesis and biological investigations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.06 | 6.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL429950 | — | — | 1 | 6.75 |
| CHEMBL417979 | — | — | 1 | 6.70 |
| CHEMBL10650 | — | — | 1 | 6.40 |
| CHEMBL274764 | — | — | 1 | 4.39 |
| CHEMBL10717 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL429950 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL417979 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL10650 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL274764 | — | IC50 | = | 40500.0 | nM | 4.39 |
| CHEMBL10717 | — | IC50 | 26800.0 | nM | - |