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Assay Detail

CHEMBL801740

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Binding
Affinity against Renal peptide transporter PepT2 in SKPT cells was measured by the inhibition of [14C]Gly-Sar uptake
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type SKPT
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 8 4.73 4.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL429950 1 4.88
CHEMBL417979 1 4.84
CHEMBL10650 1 4.73
CHEMBL1727 CEPHALEXIN ANHYDROUS 4.0 1 4.45
CHEMBL274764 1 -
CHEMBL10729 1 -
CHEMBL10717 1 -
CHEMBL269212 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL429950 Ki = 13100.0 nM 4.88
CHEMBL417979 Ki = 14600.0 nM 4.84
CHEMBL10650 Ki = 18800.0 nM 4.73
CHEMBL1727 CEPHALEXIN ANHYDROUS Ki = 35200.0 nM 4.45
CHEMBL274764 Ki = 1349000.0 nM -
CHEMBL10729 Ki = 6921000.0 nM -
CHEMBL10717 Ki = 3480000.0 nM -
CHEMBL269212 Ki = 7451000.0 nM -