PubChem structure–activity relationship (SAR) clusters

Table 5 Comparison of assays targeting aryl hydrocarbon receptor (AhR, GI 29337198)

AID	Assay methods	Ligand concentration (μM)	Activity measure	Number of compounds
AID	Assay methods	Ligand concentration (μM)	Activity measure	Tested	Active	Inactive	Unspecified	Non-inactive
PMID 19719119
431863	LRGA		Fold change	7	0	0	7	7
431864	LRGA^a	0.001	NA	1	0	1	0	0
431865	LRGA^a	0.0003	NA	1	0	1	0	0
431866	LRGA^a	0.0001	NA	1	0	1	0	0
431867	LRGA^a	20	NA	1	0	1	0	0
431868	WBA	20	NA	2	2	0	0	2
431869	WBA	20	NA	2	2	0	0	2
431870	MA	20	NA	2	2	0	0	2
PMID 20392544
490160	EROD	10	Fold change	15	0	0	15	15
490161	EROD	25	Fold change	10	0	0	10	10
490162	EROD	5	Fold change	4	0	0	4	4
490163	EROD	1	Fold change	3	0	0	3	3
PMID 21958547
631103	CALUX	?	EC₅₀	5	1	0	4	4

LRGA AhRE/XRE-luciferase reporter gene assay, EROD ethoxyresofurin-O-deethylase assay, CALUX CALUX transactivational assay, WBA western blot analysis, MA microscopic analysis with DAPI staining.
^aIn the presence of 6-hydroxy-7-methoxyflavone, which is an AhR antagonist.

ISSN: 1758-2946