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Assay Detail

CHEMBL3865063

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

Binding
Inhibition of ATX in human plasma assessed as decrease in hydrolysis of lysophosphatidylcholine by measuring choline release after 24 hrs by horseradish peroxidase/choline oxidase-coupled assay
24
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Autotaxin (CHEMBL3691)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent inhibitors of the lysophospholipase autotaxin.
Shah P, Cheasty A, Foxton C, Raynham T, Farooq M, Gutierrez IF, Lejeune A, Pritchard M, Turnbull A, Pang L, Owen P, Boyd S, Stowell A, Jordan A, Hamilton NM, Hitchin JR, Stockley M, MacDonald E, Quesada MJ, Trivier E, Skeete J, Ovaa H, Moolenaar WH, Ryder H.
Bioorg Med Chem Lett (2016) 26 : 5403 -5410
PubMed 27780639 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.55 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3917975 CAMBRITAXESTAT 2.0 1 7.85
CHEMBL3889955 1 7.80
CHEMBL3917466 1 7.72
CHEMBL3926932 1 7.58
CHEMBL3982059 1 7.50
CHEMBL3912114 1 7.47
CHEMBL3946146 1 7.36
CHEMBL3983022 1 7.00
CHEMBL3964183 2 6.75
CHEMBL3944813 1 6.67
CHEMBL3916907 1 6.54
CHEMBL3186509 1 6.54
CHEMBL3907905 1 6.50
CHEMBL3934551 1 6.48
CHEMBL3907343 1 6.38
CHEMBL3916898 1 6.35
CHEMBL3954360 1 6.09
CHEMBL3945659 1 5.98
CHEMBL3899987 1 5.48
CHEMBL3953575 1 5.24
CHEMBL3935870 1 5.07
CHEMBL1889181 1 5.05
CHEMBL3965701 1 5.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3917975 CAMBRITAXESTAT IC50 = 14.0 nM 7.85
CHEMBL3889955 IC50 = 16.0 nM 7.80
CHEMBL3917466 IC50 = 19.0 nM 7.72
CHEMBL3926932 IC50 = 26.0 nM 7.58
CHEMBL3982059 IC50 = 32.0 nM 7.50
CHEMBL3912114 IC50 = 34.0 nM 7.47
CHEMBL3946146 IC50 = 44.0 nM 7.36
CHEMBL3983022 IC50 = 99.0 nM 7.00
CHEMBL3964183 IC50 = 178.0 nM 6.75
CHEMBL3964183 IC50 = 207.0 nM 6.68
CHEMBL3944813 IC50 = 215.0 nM 6.67
CHEMBL3186509 IC50 = 289.0 nM 6.54
CHEMBL3916907 IC50 = 288.0 nM 6.54
CHEMBL3907905 IC50 = 318.0 nM 6.50
CHEMBL3934551 IC50 = 333.0 nM 6.48
CHEMBL3907343 IC50 = 414.0 nM 6.38
CHEMBL3916898 IC50 = 444.0 nM 6.35
CHEMBL3954360 IC50 = 821.0 nM 6.09
CHEMBL3945659 IC50 = 1050.0 nM 5.98
CHEMBL3899987 IC50 = 3294.0 nM 5.48
CHEMBL3953575 IC50 = 5800.0 nM 5.24
CHEMBL3935870 IC50 = 8500.0 nM 5.07
CHEMBL1889181 IC50 = 8870.0 nM 5.05
CHEMBL3965701 IC50 = 9700.0 nM 5.01