Assay Detail
Binding
CHEMBL876384
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Affinity for hPEPT1 in mature Caco-2 cell monolayers using [14C]-Gly-Sar
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 | Expert |
Publication
Dipeptidomimetic ketomethylene isosteres as pro-moieties for drug transport via the human intestinal di-/tripeptide transporter hPEPT1: design, synthesis, stability, and biological investigations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 4.45 | 4.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL188947 | — | — | 1 | 4.72 |
| CHEMBL189777 | — | — | 1 | 4.17 |
| CHEMBL187172 | — | — | 1 | - |
| CHEMBL189248 | — | — | 1 | - |
| CHEMBL434541 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL188947 | — | Ki | = | 19000.0 | nM | 4.72 |
| CHEMBL189777 | — | Ki | = | 68000.0 | nM | 4.17 |
| CHEMBL187172 | — | Ki | = | 905000.0 | nM | - |
| CHEMBL189248 | — | Ki | = | 133000.0 | nM | - |
| CHEMBL434541 | — | Ki | = | 417000.0 | nM | - |