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Assay Detail

CHEMBL4482188

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Binding
Inhibition of OAT3 (unknown origin) expressed in HEK293 cells assessed as reduction in 6-CF uptake measured after 5 mins by fluorescence assay
15
Total Activities
8
Compounds Tested
2
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

Organic anion transporter 3 (CHEMBL1641348)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dihydrophenanthrenes from Juncus effusus as Inhibitors of OAT1 and OAT3.
Li X, Qiao Y, Wang X, Ma R, Li T, Zhang Y, Borris RP.
J Nat Prod (2019) 82 : 832 -839
PubMed 30892891 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.49 5.96
Inhibition 7 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4519013 2 5.96
CHEMBL4562825 2 5.96
CHEMBL4584575 2 5.89
CHEMBL4527448 2 5.64
CHEMBL4582456 2 5.55
CHEMBL38650 2 5.19
CHEMBL4525573 2 5.08
CHEMBL205119 EFFUSOL 1 4.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4519013 IC50 = 1100.0 nM 5.96
CHEMBL4562825 IC50 = 1100.0 nM 5.96
CHEMBL4584575 IC50 = 1300.0 nM 5.89
CHEMBL4527448 IC50 = 2300.0 nM 5.64
CHEMBL4582456 IC50 = 2800.0 nM 5.55
CHEMBL38650 IC50 = 6500.0 nM 5.19
CHEMBL4525573 IC50 = 8300.0 nM 5.08
CHEMBL205119 EFFUSOL IC50 = 22700.0 nM 4.64
CHEMBL4584575 Inhibition - % -
CHEMBL4519013 Inhibition - % -
CHEMBL4582456 Inhibition - % -
CHEMBL38650 Inhibition - % -
CHEMBL4562825 Inhibition - % -
CHEMBL4525573 Inhibition - % -
CHEMBL4527448 Inhibition - % -