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Assay Detail

CHEMBL4046326

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

Binding
Inhibition of human OCT2 expressed in HEK293 cells assessed as decrease in uptake of substrate [3H]MPP+ after 1 min by liquid scintillation counting method
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Solute carrier family 22 member 2 (CHEMBL1743122)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A new chemotype inhibitor for the human organic cation transporter 3 (hOCT3).
Pan X, Iyer KA, Liu H, Sweet DH, Dukat M.
Bioorg Med Chem Lett (2017) 27 : 4440 -4445
PubMed 28811134 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.64 5.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4100146 1 5.36
CHEMBL4062501 1 5.08
CHEMBL43415 1 5.03
CHEMBL1160763 1 4.95
CHEMBL41040 1 4.72
CHEMBL1160766 1 4.32
CHEMBL13823 1 4.22
CHEMBL14047 PHENYLGUANIDINE 1 4.05
CHEMBL272259 1 4.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4100146 IC50 = 4400.0 nM 5.36
CHEMBL4062501 IC50 = 8300.0 nM 5.08
CHEMBL43415 IC50 = 9300.0 nM 5.03
CHEMBL1160763 IC50 = 11300.0 nM 4.95
CHEMBL41040 IC50 = 18900.0 nM 4.72
CHEMBL1160766 IC50 = 48300.0 nM 4.32
CHEMBL13823 IC50 = 60500.0 nM 4.22
CHEMBL14047 PHENYLGUANIDINE IC50 = 89000.0 nM 4.05
CHEMBL272259 IC50 = 96200.0 nM 4.02