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Assay Detail

CHEMBL5393050

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

Toxicity
Agonist activity at Niacin receptor (unknown origin)
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Toxicity
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Hydroxycarboxylic acid receptor 2 (CHEMBL3785)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tuning the Reactivity of Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) Activators for Optimal <i>in Vivo</i> Efficacy.
Markovtsov V, Duncton MAJ, Bagos A, Yi S, Braselmann S, Bhamidipati S, Darwish IS, Yu J, Owyang AM, Fernandez B, Samant B, Park G, Masuda ES, Shaw SJ.
ACS Med Chem Lett (2023) 14 : 1700 -1706
PubMed 38116420 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.96 9.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL589586 MONOMETHYL FUMARATE 4.0 1 9.02
CHEMBL2107333 DIMETHYL FUMARATE 4.0 1 6.89
CHEMBL5415198 1 -
CHEMBL5393772 1 -
CHEMBL5408914 1 -
CHEMBL5430762 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL589586 MONOMETHYL FUMARATE IC50 = 0.96 nM 9.02
CHEMBL2107333 DIMETHYL FUMARATE IC50 = 130.0 nM 6.89
CHEMBL5415198 IC50 > 1000.0 nM -
CHEMBL5393772 IC50 > 1000.0 nM -
CHEMBL5408914 IC50 > 1000.0 nM -
CHEMBL5430762 IC50 > 1000.0 nM -