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Assay Detail

CHEMBL863210

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Activation of human PEPT1 expressed in MDCK cells
80
Total Activities
80
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

Target

Solute carrier family 15 member 1 (CHEMBL4605)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Human PEPT1 pharmacophore distinguishes between dipeptide transport and binding.
Vig BS, Stouch TR, Timoszyk JK, Quan Y, Wall DA, Smith RL, Faria TN.
J Med Chem (2006) 49 : 3636 -3644
PubMed 16759105 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 80 4.20 4.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL378907 1 4.52
CHEMBL108438 1 4.52
CHEMBL91777 VALYLTRYPTOPHAN 1 4.40
CHEMBL39159 1 4.30
CHEMBL95286 1 4.22
CHEMBL94016 1 4.22
CHEMBL54552 VAL-VAL 1 4.16
CHEMBL54933 LEU-LEU 1 4.10
CHEMBL17697 1 4.10
CHEMBL57338 1 4.10
CHEMBL91792 1 4.10
CHEMBL438960 1 4.00
CHEMBL316103 1 4.00
CHEMBL188866 1 4.00
CHEMBL91241 1 -
CHEMBL175737 GLYCYLSARCOSINE 1 -
CHEMBL80548 GLYCYL PROLINE 1 -
CHEMBL378267 1 -
CHEMBL299889 1 -
CHEMBL210850 1 -
CHEMBL209670 GLYCYLLEUCYLPHENYLALANINE 1 -
CHEMBL209341 1 -
CHEMBL56119 1 -
CHEMBL93127 1 -
CHEMBL420061 1 -
CHEMBL378905 1 -
CHEMBL91392 1 -
CHEMBL314532 1 -
CHEMBL54278 GLYCYLGLYCYLGLYCINE 1 -
CHEMBL292467 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL378907 EC50 = 30000.0 nM 4.52
CHEMBL108438 EC50 = 30000.0 nM 4.52
CHEMBL91777 VALYLTRYPTOPHAN EC50 = 40000.0 nM 4.40
CHEMBL39159 EC50 = 50000.0 nM 4.30
CHEMBL95286 EC50 = 60000.0 nM 4.22
CHEMBL94016 EC50 = 60000.0 nM 4.22
CHEMBL54552 VAL-VAL EC50 = 70000.0 nM 4.16
CHEMBL54933 LEU-LEU EC50 = 80000.0 nM 4.10
CHEMBL17697 EC50 = 80000.0 nM 4.10
CHEMBL57338 EC50 = 80000.0 nM 4.10
CHEMBL91792 EC50 = 80000.0 nM 4.10
CHEMBL438960 EC50 = 100000.0 nM 4.00
CHEMBL316103 EC50 = 100000.0 nM 4.00
CHEMBL188866 EC50 = 100000.0 nM 4.00
CHEMBL421361 EC50 = 510000.0 nM -
CHEMBL377325 EC50 - -
CHEMBL318315 EC50 = 1000000.0 nM -
CHEMBL377872 EC50 = 370000.0 nM -
CHEMBL441685 EC50 = 690000.0 nM -
CHEMBL210490 EC50 = 470000.0 nM -
CHEMBL421171 EC50 = 440000.0 nM -
CHEMBL17171 EC50 = 990000.0 nM -
CHEMBL380024 EC50 - -
CHEMBL382777 EC50 = 270000.0 nM -
CHEMBL296756 EC50 - -
CHEMBL191057 EC50 = 220000.0 nM -
CHEMBL380047 EC50 = 230000.0 nM -
CHEMBL210784 EC50 - -
CHEMBL286852 EC50 - -
CHEMBL190027 EC50 > 5000000.0 nM -
CHEMBL59426 EC50 - -
CHEMBL293494 EC50 = 250000.0 nM -
CHEMBL209341 EC50 = 210000.0 nM -
CHEMBL292467 EC50 = 480000.0 nM -
CHEMBL54278 GLYCYLGLYCYLGLYCINE EC50 = 580000.0 nM -
CHEMBL314532 EC50 = 1100000.0 nM -
CHEMBL91392 EC50 = 550000.0 nM -
CHEMBL378905 EC50 - -
CHEMBL420061 EC50 = 750000.0 nM -
CHEMBL93127 EC50 = 400000.0 nM -
CHEMBL56119 EC50 = 170000.0 nM -
CHEMBL190361 EC50 = 310000.0 nM -
CHEMBL209670 GLYCYLLEUCYLPHENYLALANINE EC50 = 280000.0 nM -
CHEMBL210850 EC50 = 420000.0 nM -
CHEMBL299889 EC50 = 130000.0 nM -
CHEMBL378267 EC50 - -
CHEMBL80548 GLYCYL PROLINE EC50 = 130000.0 nM -
CHEMBL175737 GLYCYLSARCOSINE EC50 = 540000.0 nM -
CHEMBL91241 EC50 = 520000.0 nM -
CHEMBL773 GLYCINE EC50 - -