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Assay Detail

CHEMBL4040574

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

Binding
Inhibition of glycosylated human ATX using FS-3 as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by fluorescence assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Autotaxin (CHEMBL3691)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery, Structure-Activity Relationship, and Binding Mode of an Imidazo[1,2-a]pyridine Series of Autotaxin Inhibitors.
Joncour A, Desroy N, Housseman C, Bock X, Bienvenu N, Cherel L, Labeguere V, Peixoto C, Annoot D, Lepissier L, Heiermann J, Hengeveld WJ, Pilzak G, Monjardet A, Wakselman E, Roncoroni V, Le Tallec S, Galien R, David C, Vandervoort N, Christophe T, Conrath K, Jans M, Wohlkonig A, Soror S, Steyaert J, Touitou R, Fleury D, Vercheval L, Mollat P, Triballeau N, van der Aar E, Brys R, Heckmann B.
J Med Chem (2017) 60 : 7371 -7392
PubMed 28731719 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.94 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4100462 1 8.70
CHEMBL4073638 1 8.30
CHEMBL4084005 1 8.10
CHEMBL4062291 1 8.05
CHEMBL4091774 1 7.92
CHEMBL4061747 1 7.57
CHEMBL4084750 1 6.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4100462 IC50 = 2.0 nM 8.70
CHEMBL4073638 IC50 = 5.0 nM 8.30
CHEMBL4084005 IC50 = 8.0 nM 8.10
CHEMBL4062291 IC50 = 9.0 nM 8.05
CHEMBL4091774 IC50 = 12.0 nM 7.92
CHEMBL4061747 IC50 = 27.0 nM 7.57
CHEMBL4084750 IC50 = 122.0 nM 6.91