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Assay Detail

CHEMBL4714710

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

Binding
Inhibition of recombinant human C-terminal His6-tagged ATX expressed in baculovirus infected Sf21 insect cells using LPC as substrate incubated for 2 hrs by rapidFire based MS/MS analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf21
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Autotaxin (CHEMBL3691)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel Pyridazines as Autotaxin Inhibitors for Treating Inflammatory Airway or Fibrotic Diseases.
Sabnis RW.
ACS Med Chem Lett (2021) 12 : 528 -529
PubMed 33859788 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.76 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4788435 1 8.82
CHEMBL4745566 1 8.80
CHEMBL4758133 1 8.74
CHEMBL4751395 1 8.74
CHEMBL4743845 1 8.72
CHEMBL4784419 1 8.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4788435 IC50 = 1.5 nM 8.82
CHEMBL4745566 IC50 = 1.6 nM 8.80
CHEMBL4758133 IC50 = 1.8 nM 8.74
CHEMBL4751395 IC50 = 1.8 nM 8.74
CHEMBL4743845 IC50 = 1.9 nM 8.72
CHEMBL4784419 IC50 = 1.9 nM 8.72