Assay Detail
Functional
CHEMBL863213
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human PEPT1 assessed as inhibition of [14C]Gly-Sar uptake in MDCK cells
81
Total Activities
81
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | MDCK |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Human PEPT1 pharmacophore distinguishes between dipeptide transport and binding.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 81 | 4.17 | 4.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL378907 | — | — | 1 | 4.70 |
| CHEMBL95286 | — | — | 1 | 4.22 |
| CHEMBL56119 | — | — | 1 | 4.16 |
| CHEMBL57338 | — | — | 1 | 4.16 |
| CHEMBL429950 | — | — | 1 | 4.16 |
| CHEMBL39179 | — | — | 1 | 4.10 |
| CHEMBL108438 | — | — | 1 | 4.10 |
| CHEMBL39159 | — | — | 1 | 4.05 |
| CHEMBL91777 | VALYLTRYPTOPHAN | — | 1 | 4.00 |
| CHEMBL210851 | — | — | 1 | 4.00 |
| CHEMBL93127 | — | — | 1 | - |
| CHEMBL378267 | — | — | 1 | - |
| CHEMBL318315 | — | — | 1 | - |
| CHEMBL209341 | — | — | 1 | - |
| CHEMBL209670 | GLYCYLLEUCYLPHENYLALANINE | — | 1 | - |
| CHEMBL420061 | — | — | 1 | - |
| CHEMBL299889 | — | — | 1 | - |
| CHEMBL380024 | — | — | 1 | - |
| CHEMBL210784 | — | — | 1 | - |
| CHEMBL17697 | — | — | 1 | - |
| CHEMBL340564 | — | — | 1 | - |
| CHEMBL54278 | GLYCYLGLYCYLGLYCINE | — | 1 | - |
| CHEMBL292467 | — | — | 1 | - |
| CHEMBL314532 | — | — | 1 | - |
| CHEMBL91392 | — | — | 1 | - |
| CHEMBL91241 | — | — | 1 | - |
| CHEMBL773 | GLYCINE | 4.0 | 1 | - |
| CHEMBL80548 | GLYCYL PROLINE | — | 1 | - |
| CHEMBL175737 | GLYCYLSARCOSINE | — | 1 | - |
| CHEMBL378905 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL378907 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL95286 | — | IC50 | = | 60000.0 | nM | 4.22 |
| CHEMBL56119 | — | IC50 | = | 70000.0 | nM | 4.16 |
| CHEMBL57338 | — | IC50 | = | 70000.0 | nM | 4.16 |
| CHEMBL429950 | — | IC50 | = | 70000.0 | nM | 4.16 |
| CHEMBL39179 | — | IC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL108438 | — | IC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL39159 | — | IC50 | = | 90000.0 | nM | 4.05 |
| CHEMBL91777 | VALYLTRYPTOPHAN | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL210851 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL421171 | — | IC50 | = | 810000.0 | nM | - |
| CHEMBL17171 | — | IC50 | = | 630000.0 | nM | - |
| CHEMBL190361 | — | IC50 | = | 720000.0 | nM | - |
| CHEMBL382777 | — | IC50 | = | 390000.0 | nM | - |
| CHEMBL296756 | — | IC50 | = | 7310000.0 | nM | - |
| CHEMBL94016 | — | IC50 | = | 170000.0 | nM | - |
| CHEMBL91792 | — | IC50 | = | 260000.0 | nM | - |
| CHEMBL191057 | — | IC50 | = | 280000.0 | nM | - |
| CHEMBL371194 | — | IC50 | = | 800000.0 | nM | - |
| CHEMBL380047 | — | IC50 | = | 450000.0 | nM | - |
| CHEMBL210490 | — | IC50 | = | 1310000.0 | nM | - |
| CHEMBL441685 | — | IC50 | = | 310000.0 | nM | - |
| CHEMBL438960 | — | IC50 | = | 150000.0 | nM | - |
| CHEMBL210850 | — | IC50 | = | 510000.0 | nM | - |
| CHEMBL377872 | — | IC50 | = | 400000.0 | nM | - |
| CHEMBL421361 | — | IC50 | = | 390000.0 | nM | - |
| CHEMBL286852 | — | IC50 | = | 250000.0 | nM | - |
| CHEMBL59426 | — | IC50 | > | 16000000.0 | nM | - |
| CHEMBL293494 | — | IC50 | = | 620000.0 | nM | - |
| CHEMBL377325 | — | IC50 | > | 16000000.0 | nM | - |
| CHEMBL340564 | — | IC50 | - | — | - | |
| CHEMBL378905 | — | IC50 | - | — | - | |
| CHEMBL175737 | GLYCYLSARCOSINE | IC50 | = | 1160000.0 | nM | - |
| CHEMBL80548 | GLYCYL PROLINE | IC50 | = | 330000.0 | nM | - |
| CHEMBL773 | GLYCINE | IC50 | - | — | - | |
| CHEMBL91241 | — | IC50 | = | 1820000.0 | nM | - |
| CHEMBL91392 | — | IC50 | = | 380000.0 | nM | - |
| CHEMBL314532 | — | IC50 | = | 650000.0 | nM | - |
| CHEMBL292467 | — | IC50 | = | 820000.0 | nM | - |
| CHEMBL54278 | GLYCYLGLYCYLGLYCINE | IC50 | = | 1070000.0 | nM | - |
| CHEMBL17697 | — | IC50 | = | 250000.0 | nM | - |
| CHEMBL93127 | — | IC50 | = | 810000.0 | nM | - |
| CHEMBL378267 | — | IC50 | - | — | - | |
| CHEMBL318315 | — | IC50 | = | 620000.0 | nM | - |
| CHEMBL209341 | — | IC50 | = | 240000.0 | nM | - |
| CHEMBL209670 | GLYCYLLEUCYLPHENYLALANINE | IC50 | = | 980000.0 | nM | - |
| CHEMBL420061 | — | IC50 | = | 1250000.0 | nM | - |
| CHEMBL299889 | — | IC50 | = | 170000.0 | nM | - |
| CHEMBL380024 | — | IC50 | = | 8110000.0 | nM | - |
| CHEMBL210784 | — | IC50 | - | — | - |