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Assay Detail

CHEMBL3744704

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

Binding
Inhibition of recombinant human PTP-sigma (residues 1367 to 1948) using para-nitrophenylphosphate as substrate for 60 mins by fluorescence analysis
30
Total Activities
30
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

Receptor-type tyrosine-protein phosphatase S (CHEMBL2396508)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of novel protein tyrosine phosphatase sigma inhibitors promoting neurite extension.
Lee HS, Ku B, Park TH, Park H, Choi JK, Chang KT, Kim CH, Ryu SE, Kim SJ.
Bioorg Med Chem Lett (2016) 26 : 87 -93
PubMed 26602279 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 5.49 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1438439 IRIGENOL 1 6.30
CHEMBL55415 SCUTELLAREIN 1 6.22
CHEMBL3739950 1 6.10
CHEMBL3740878 1 6.05
CHEMBL398328 1 5.52
CHEMBL28626 MORIN 1 5.37
CHEMBL3740356 1 5.27
CHEMBL3739990 1 5.18
CHEMBL179166 SODIUM ORTHOVANAD 1 5.08
CHEMBL8260 BAICALEIN 2.0 1 4.99
CHEMBL3741920 1 4.98
CHEMBL247484 TRICETIN 1 4.76
CHEMBL3742081 1 -
CHEMBL3739546 1 -
CHEMBL309263 1 -
CHEMBL3741913 1 -
CHEMBL3288727 1 -
CHEMBL3742073 1 -
CHEMBL3741139 1 -
CHEMBL3742307 1 -
CHEMBL241609 OROBOL 1 -
CHEMBL3741744 1 -
CHEMBL1950539 1 -
CHEMBL3740337 1 -
CHEMBL3741864 1 -
CHEMBL3740766 1 -
CHEMBL3739836 1 -
CHEMBL3741052 1 -
CHEMBL150 KAEMPFEROL 1.0 1 -
CHEMBL3740881 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1438439 IRIGENOL IC50 = 500.0 nM 6.30
CHEMBL55415 SCUTELLAREIN IC50 = 600.0 nM 6.22
CHEMBL3739950 IC50 = 800.0 nM 6.10
CHEMBL3740878 IC50 = 900.0 nM 6.05
CHEMBL398328 IC50 = 3000.0 nM 5.52
CHEMBL28626 MORIN IC50 = 4300.0 nM 5.37
CHEMBL3740356 IC50 = 5400.0 nM 5.27
CHEMBL3739990 IC50 = 6600.0 nM 5.18
CHEMBL179166 SODIUM ORTHOVANAD IC50 = 8300.0 nM 5.08
CHEMBL8260 BAICALEIN IC50 = 10300.0 nM 4.99
CHEMBL3741920 IC50 = 10400.0 nM 4.98
CHEMBL247484 TRICETIN IC50 = 17500.0 nM 4.76
CHEMBL3742081 IC50 - -
CHEMBL3739546 IC50 - -
CHEMBL309263 IC50 - -
CHEMBL3741913 IC50 - -
CHEMBL3288727 IC50 - -
CHEMBL3742073 IC50 - -
CHEMBL3741139 IC50 - -
CHEMBL3742307 IC50 - -
CHEMBL241609 OROBOL IC50 - -
CHEMBL3741744 IC50 - -
CHEMBL1950539 IC50 - -
CHEMBL3740337 IC50 - -
CHEMBL3741864 IC50 - -
CHEMBL3740766 IC50 - -
CHEMBL3739836 IC50 - -
CHEMBL3741052 IC50 - -
CHEMBL150 KAEMPFEROL IC50 - -
CHEMBL3740881 IC50 - -