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Assay Detail

CHEMBL3591334

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

Binding
Displacement of [3H]-nicotinic acid from N-flag-tagged human HCA2 receptor expressed in HEK293T cell membranes by scintillation counting analysis
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Affinity and kinetics study of anthranilic acids as HCA2 receptor agonists.
van Veldhoven JP, Liu R, Thee SA, Wouters Y, Verhoork SJ, Mooiman C, Louvel J, IJzerman AP.
Bioorg Med Chem (2015) 23 : 4013 -4025
PubMed 25737085 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.73 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3589834 1 7.64
CHEMBL235256 1 7.47
CHEMBL3589835 1 7.24
CHEMBL1085711 1 7.12
CHEMBL3589788 1 7.08
CHEMBL3589790 1 7.07
CHEMBL3589793 1 7.04
CHEMBL1083473 1 7.03
CHEMBL3589837 1 6.98
CHEMBL3589836 1 6.97
CHEMBL3589833 1 6.89
CHEMBL3589791 1 6.70
CHEMBL573 NIACIN 4.0 1 6.60
CHEMBL3589785 1 6.55
CHEMBL235741 1 6.54
CHEMBL3589789 1 6.49
CHEMBL3589779 1 6.49
CHEMBL3589792 1 6.44
CHEMBL3589787 1 6.26
CHEMBL3589783 1 6.11
CHEMBL3589782 1 6.10
CHEMBL3589786 1 6.03
CHEMBL3589784 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3589834 IC50 = 23.0 nM 7.64
CHEMBL235256 IC50 = 34.0 nM 7.47
CHEMBL3589835 IC50 = 58.0 nM 7.24
CHEMBL1085711 IC50 = 75.0 nM 7.12
CHEMBL3589788 IC50 = 83.0 nM 7.08
CHEMBL3589790 IC50 = 86.0 nM 7.07
CHEMBL3589793 IC50 = 91.0 nM 7.04
CHEMBL1083473 IC50 = 94.0 nM 7.03
CHEMBL3589837 IC50 = 105.0 nM 6.98
CHEMBL3589836 IC50 = 108.0 nM 6.97
CHEMBL3589833 IC50 = 129.0 nM 6.89
CHEMBL3589791 IC50 = 201.0 nM 6.70
CHEMBL573 NIACIN IC50 = 249.0 nM 6.60
CHEMBL3589785 IC50 = 283.0 nM 6.55
CHEMBL235741 IC50 = 290.0 nM 6.54
CHEMBL3589789 IC50 = 326.0 nM 6.49
CHEMBL3589779 IC50 = 323.0 nM 6.49
CHEMBL3589792 IC50 = 365.0 nM 6.44
CHEMBL3589787 IC50 = 555.0 nM 6.26
CHEMBL3589783 IC50 = 769.0 nM 6.11
CHEMBL3589782 IC50 = 800.0 nM 6.10
CHEMBL3589786 IC50 = 940.0 nM 6.03
CHEMBL3589784 IC50 = 1401.0 nM 5.85