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Assay Detail

CHEMBL4433170

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

Binding
Inhibition of autotaxin in healthy human whole blood assessed as reduction in LPA level after 2 hrs by LC-MS/MS analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Autotaxin (CHEMBL3691)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel Autotaxin Inhibitors for the Treatment of Osteoarthritis Pain: Lead Optimization via Structure-Based Drug Design.
Jones SB, Pfeifer LA, Bleisch TJ, Beauchamp TJ, Durbin JD, Klimkowski VJ, Hughes NE, Rito CJ, Dao Y, Gruber JM, Bui H, Chambers MG, Chandrasekhar S, Lin C, McCann DJ, Mudra DR, Oskins JL, Swearingen CA, Thirunavukkarasu K, Norman BH.
ACS Med Chem Lett (2016) 7 : 857 -861
PubMed 27660691 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.00 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3186509 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3186509 IC50 = 100.0 nM 7.00