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Assay Detail

CHEMBL4616525

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

Binding
Inhibition of human ATX by LPC choline release assay
3
Total Activities
3
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 of Novel Indole-Based Allosteric Highly Potent ATX Inhibitors with Great In Vivo Efficacy in a Mouse Lung Fibrosis Model.
Lei H, Guo M, Li X, Jia F, Li C, Yang Y, Cao M, Jiang N, Ma E, Zhai X.
J Med Chem (2020) 63 : 7326 -7346
PubMed 32479084 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.05 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4086925 1 7.22
CHEMBL3828074 ZIRITAXESTAT 3.0 1 6.88
CHEMBL4642052 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4086925 IC50 = 60.0 nM 7.22
CHEMBL3828074 ZIRITAXESTAT IC50 = 131.0 nM 6.88
CHEMBL4642052 IC50 < 500.0 nM -