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Assay Detail

CHEMBL2077082

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

Functional
TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in rOAT3-expressing S2 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type S2
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Organic anion transporter 3 (CHEMBL2073666)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine.
Khamdang S, Takeda M, Shimoda M, Noshiro R, Narikawa S, Huang XL, Enomoto A, Piyachaturawat P, Endou H.
J Pharmacol Sci (2004) 94 : 197 -202
PubMed 14978359 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.78 5.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL897 PROBENECID 4.0 1 5.22
CHEMBL1144 PRAVASTATIN 4.0 1 4.81
CHEMBL1231530 BETAMIPRON 2.0 1 4.32
CHEMBL30 CIMETIDINE 4.0 1 -
CHEMBL766 CILASTATIN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL897 PROBENECID IC50 = 6030.0 nM 5.22
CHEMBL1144 PRAVASTATIN IC50 = 15600.0 nM 4.81
CHEMBL1231530 BETAMIPRON IC50 = 47500.0 nM 4.32
CHEMBL30 CIMETIDINE IC50 = 166000.0 nM -
CHEMBL766 CILASTATIN IC50 = 742000.0 nM -