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Assay Detail

CHEMBL4833047

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

Binding
Inhibition of human recombinant PTP1B (1 to 322 residues) expressed in Escherichia coli using pNPP as substrate preincubated with substrate for 10 mins followed by enzyme addition and measured for 10 mins by absorbance based analysis
14
Total Activities
14
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

Dual High-Resolution α-Glucosidase and PTP1B Inhibition Profiling Combined with HPLC-PDA-HRMS-SPE-NMR Analysis for the Identification of Potentially Antidiabetic Chromene Meroterpenoids from <i>Rhododendron capitatum</i>.
Liang C, Kjaerulff L, Hansen PR, Kongstad KT, Staerk D.
J Nat Prod (2021) 84 : 2454 -2467
PubMed 34460246 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.02 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL508583 TRODUSQUEMINE 2.0 1 6.00
CHEMBL184041 ERTIPROTAFIB 2.0 1 5.80
CHEMBL2310311 1 5.60
CHEMBL513978 GRIFOLIC ACID 1 5.44
CHEMBL4866095 1 5.22
CHEMBL4876070 1 4.99
CHEMBL4856719 1 4.70
CHEMBL4847372 1 4.55
CHEMBL4849561 1 4.44
CHEMBL4854129 1 4.27
CHEMBL4859368 1 4.17
CHEMBL168 OLEANOLIC_ACID 1 -
CHEMBL169 URSOLIC ACID 2.0 1 -
CHEMBL4874393 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL508583 TRODUSQUEMINE IC50 = 1000.0 nM 6.00
CHEMBL184041 ERTIPROTAFIB IC50 = 1600.0 nM 5.80
CHEMBL2310311 IC50 = 2500.0 nM 5.60
CHEMBL513978 GRIFOLIC ACID IC50 = 3600.0 nM 5.44
CHEMBL4866095 IC50 = 6000.0 nM 5.22
CHEMBL4876070 IC50 = 10300.0 nM 4.99
CHEMBL4856719 IC50 = 19900.0 nM 4.70
CHEMBL4847372 IC50 = 28200.0 nM 4.55
CHEMBL4849561 IC50 = 36300.0 nM 4.44
CHEMBL4854129 IC50 = 53600.0 nM 4.27
CHEMBL4859368 IC50 = 68100.0 nM 4.17
CHEMBL168 OLEANOLIC_ACID IC50 - -
CHEMBL169 URSOLIC ACID IC50 - -
CHEMBL4874393 IC50 - -