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Assay Detail

CHEMBL4038757

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 by Dixon plot analysis
9
Total Activities
9
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

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
Ki 9 5.88 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL555017 GAMBOGIC ACID 1 6.72
CHEMBL4095800 1 6.52
CHEMBL4069859 1 6.41
CHEMBL2205166 GAMBOGENIC ACID 1 5.92
CHEMBL4068566 1 5.83
CHEMBL4090412 1 5.76
CHEMBL4059800 1 5.36
CHEMBL4068458 1 4.53
CHEMBL169 URSOLIC ACID 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL555017 GAMBOGIC ACID Ki = 190.0 nM 6.72
CHEMBL4095800 Ki = 300.0 nM 6.52
CHEMBL4069859 Ki = 390.0 nM 6.41
CHEMBL2205166 GAMBOGENIC ACID Ki = 1210.0 nM 5.92
CHEMBL4068566 Ki = 1490.0 nM 5.83
CHEMBL4090412 Ki = 1750.0 nM 5.76
CHEMBL4059800 Ki = 4380.0 nM 5.36
CHEMBL4068458 Ki = 29260.0 nM 4.53
CHEMBL169 URSOLIC ACID Ki - -