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Assay Detail

CHEMBL4038754

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

Binding
Inhibition of recombinant human PTP1B (1 to 322 residues) expressed in Escherichia coli using pNPP as substrate incubated for 10 mins measured for 30 mins by spectrometric analysis
18
Total Activities
10
Compounds Tested
2
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

Competitive protein tyrosine phosphatase 1B (PTP1B) inhibitors, prenylated caged xanthones from Garcinia hanburyi and their inhibitory mechanism.
Tan XF, Uddin Z, Park C, Song YH, Son M, Lee KW, Park KH.
Bioorg Med Chem (2017) 25 : 2498 -2506
PubMed 28318895 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.39 6.33
Inhibition 8 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL555017 GAMBOGIC ACID 2 6.33
CHEMBL4095800 2 6.13
CHEMBL4069859 2 6.03
CHEMBL2205166 GAMBOGENIC ACID 2 5.46
CHEMBL4090412 2 5.35
CHEMBL4068566 2 5.33
CHEMBL4059800 2 4.89
CHEMBL169 URSOLIC ACID 2.0 1 4.81
CHEMBL4068458 2 4.15
CHEMBL4088075 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL555017 GAMBOGIC ACID IC50 = 470.0 nM 6.33
CHEMBL4095800 IC50 = 740.0 nM 6.13
CHEMBL4069859 IC50 = 930.0 nM 6.03
CHEMBL2205166 GAMBOGENIC ACID IC50 = 3470.0 nM 5.46
CHEMBL4090412 IC50 = 4440.0 nM 5.35
CHEMBL4068566 IC50 = 4690.0 nM 5.33
CHEMBL4059800 IC50 = 12790.0 nM 4.89
CHEMBL169 URSOLIC ACID IC50 = 15500.0 nM 4.81
CHEMBL4068458 IC50 = 70250.0 nM 4.15
CHEMBL4059800 Inhibition - % -
CHEMBL4068458 Inhibition - % -
CHEMBL4095800 Inhibition - % -
CHEMBL2205166 GAMBOGENIC ACID Inhibition - % -
CHEMBL4069859 Inhibition - % -
CHEMBL4068566 Inhibition - % -
CHEMBL4090412 Inhibition - % -
CHEMBL555017 GAMBOGIC ACID Inhibition - % -
CHEMBL4088075 IC50 > 200000.0 nM -