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Assay Detail

CHEMBL4477438

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

Binding
Inhibition of GST-tagged human PTP1B expressed in Escherichia coli using pNPP substrate assessed as reduction in p-nitrophenol release
10
Total Activities
10
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

Tyrosine-protein phosphatase non-receptor type 1 (CHEMBL335)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of PTP1B and α-Glucosidase Inhibitory Serrulatanes from Eremophila spp. by Combined use of Dual High-Resolution PTP1B and α-Glucosidase Inhibition Profiling and HPLC-HRMS-SPE-NMR.
Wubshet SG, Tahtah Y, Heskes AM, Kongstad KT, Pateraki I, Hamberger B, Møller BL, Staerk D.
J Nat Prod (2016) 79 : 1063 -1072
PubMed 26960032 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.36 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4554678 1 5.82
CHEMBL403093 OHIOENSIN A 1 5.46
CHEMBL4524583 1 5.46
CHEMBL403094 OHIOENSIN F 1 5.46
CHEMBL403411 OHIOENSIN G 1 5.46
CHEMBL4561426 1 5.26
CHEMBL4566713 1 5.23
CHEMBL2086414 RHODODENDRIC ACID A 1 5.20
CHEMBL523622 1 5.13
CHEMBL1835376 LOBOPHYTUMIN C 1 5.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4554678 IC50 = 1500.0 nM 5.82
CHEMBL403093 OHIOENSIN A IC50 = 3500.0 nM 5.46
CHEMBL4524583 IC50 = 3500.0 nM 5.46
CHEMBL403094 OHIOENSIN F IC50 = 3500.0 nM 5.46
CHEMBL403411 OHIOENSIN G IC50 = 3500.0 nM 5.46
CHEMBL4561426 IC50 = 5500.0 nM 5.26
CHEMBL4566713 IC50 = 5900.0 nM 5.23
CHEMBL2086414 RHODODENDRIC ACID A IC50 = 6300.0 nM 5.20
CHEMBL523622 IC50 = 7400.0 nM 5.13
CHEMBL1835376 LOBOPHYTUMIN C IC50 = 7800.0 nM 5.11