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Assay Detail

CHEMBL1048412

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

Binding
Noncompetitive type inhibition of human autotaxin at free state isolated from MDA-MB-231 cells assessed as blockade of FS3 substrate hydrolysis by FRET assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MDA-MB-231
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Autotaxin (CHEMBL3691)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of a pipemidic acid autotaxin inhibitor.
Hoeglund AB, Bostic HE, Howard AL, Wanjala IW, Best MD, Baker DL, Parrill AL.
J Med Chem (2010) 53 : 1056 -1066
PubMed 20041668 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 6.19 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL117021 LYSOPHOSPHATIDIC ACID 1 7.00
CHEMBL570352 1 6.70
CHEMBL570823 1 4.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL117021 LYSOPHOSPHATIDIC ACID Ki = 100.0 nM 7.00
CHEMBL570352 Ki = 200.0 nM 6.70
CHEMBL570823 Ki = 13200.0 nM 4.88