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Assay Detail

CHEMBL699707

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Binding
Affinity fo the compound against human Intestinal peptide transporter PepT1 in Caco-2 cells was measured as inhibition of [14C]Gly-Sar uptake
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

Target

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

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
Ki 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 4.40
CHEMBL10717 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL429950 Ki = 180.0 nM 6.75
CHEMBL417979 Ki = 200.0 nM 6.70
CHEMBL10650 Ki = 400.0 nM 6.40
CHEMBL274764 Ki = 39800.0 nM 4.40
CHEMBL10717 Ki 26400.0 nM -