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Assay Detail

CHEMBL3773098

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

Binding
Inhibition of NaCT in rat hepatocytes assessed as [14C]-citrate uptake after 30 mins by scintillation counting method
2
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type Hepatocyte
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Na(+)/citrate cotransporter (CHEMBL3769295)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Optimization of a Dicarboxylic Series for in Vivo Inhibition of Citrate Transport by the Solute Carrier 13 (SLC13) Family.
Huard K, Gosset JR, Montgomery JI, Gilbert A, Hayward MM, Magee TV, Cabral S, Uccello DP, Bahnck K, Brown J, Purkal J, Gorgoglione M, Lanba A, Futatsugi K, Herr M, Genung NE, Aspnes G, Polivkova J, Garcia-Irizarry CN, Li Q, Canterbury D, Niosi M, Vera NB, Li Z, Khunte B, Siderewicz J, Rolph T, Erion DM.
J Med Chem (2016) 59 : 1165 -1175
PubMed 26734723 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.91 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3771118 2 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3771118 IC50 = 120.0 nM 6.92
CHEMBL3771118 IC50 = 125.89 nM 6.90