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Assay Detail

CHEMBL3773093

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

Binding
Inhibition of NaDC1 (unknown origin) expressed in HEK293 cells assessed as inhibition of [14C]citrate uptake by microbeta plate reader analysis
3
Total Activities
2
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 13 member 2 (CHEMBL3712851)
Type SINGLE PROTEIN
Organism Homo sapiens

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 3 4.94 5.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3771118 2 5.00
CHEMBL3769578 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3771118 IC50 = 10000.0 nM 5.00
CHEMBL3771118 IC50 = 13200.0 nM 4.88
CHEMBL3769578 IC50 > 100000.0 nM -