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Assay Detail

CHEMBL801739

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Binding
Concentration required to inhibit the maximum [14C]Gly-Sar uptake by Renal peptide transporter PepT2 in SKPT cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type SKPT
Confidence 1 — Organism
Curated By Autocuration

Publication

Phe-Gly dipeptidomimetics designed for the di-/tripeptide transporters PEPT1 and PEPT2: synthesis and biological investigations.
Våbenø J, Lejon T, Nielsen CU, Steffansen B, Chen W, Ouyang H, Borchardt RT, Luthman K.
J Med Chem (2004) 47 : 1060 -1069
PubMed 14761208 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 4.65 4.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL429950 1 4.81
CHEMBL417979 1 4.76
CHEMBL10650 1 4.65
CHEMBL1727 CEPHALEXIN ANHYDROUS 4.0 1 4.38
CHEMBL274764 1 -
CHEMBL10729 1 -
CHEMBL10717 1 -
CHEMBL269212 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL429950 IC50 = 15500.0 nM 4.81
CHEMBL417979 IC50 = 17200.0 nM 4.76
CHEMBL10650 IC50 = 22200.0 nM 4.65
CHEMBL1727 CEPHALEXIN ANHYDROUS IC50 = 41600.0 nM 4.38
CHEMBL274764 IC50 = 1594000.0 nM -
CHEMBL10729 IC50 = 8176000.0 nM -
CHEMBL10717 IC50 = 4111000.0 nM -
CHEMBL269212 IC50 = 8802000.0 nM -