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Assay Detail

CHEMBL4187359

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 P-NPP as substrate after 10 mins by Dixon plot 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

Inhibition of protein tyrosine phosphatase 1B (PTP1B) and α-glucosidase by xanthones from Cratoxylum cochinchinense, and their kinetic characterization.
Li ZP, Song YH, Uddin Z, Wang Y, Park KH.
Bioorg Med Chem (2018) 26 : 737 -746
PubMed 29306546 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 5.12 5.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4211682 1 5.68
CHEMBL260553 1 5.57
CHEMBL1782241 COCHINCHINONE A 1 5.51
CHEMBL323197 MANGOSTIN 1 5.50
CHEMBL4208135 1 5.47
CHEMBL4214309 1 5.29
CHEMBL4203265 1 5.05
CHEMBL1782240 1 4.96
CHEMBL4209191 1 4.70
CHEMBL4217516 1 4.64
CHEMBL4202640 1 4.53
CHEMBL4218731 1 4.49
CHEMBL307429 DUVOGLUSTAT 2.0 1 -
CHEMBL169 URSOLIC ACID 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4211682 Ki = 2100.0 nM 5.68
CHEMBL260553 Ki = 2700.0 nM 5.57
CHEMBL1782241 COCHINCHINONE A Ki = 3100.0 nM 5.51
CHEMBL323197 MANGOSTIN Ki = 3200.0 nM 5.50
CHEMBL4208135 Ki = 3400.0 nM 5.47
CHEMBL4214309 Ki = 5100.0 nM 5.29
CHEMBL4203265 Ki = 8900.0 nM 5.05
CHEMBL1782240 Ki = 11100.0 nM 4.96
CHEMBL4209191 Ki = 19900.0 nM 4.70
CHEMBL4217516 Ki = 22900.0 nM 4.64
CHEMBL4202640 Ki = 29500.0 nM 4.53
CHEMBL4218731 Ki = 32700.0 nM 4.49
CHEMBL307429 DUVOGLUSTAT Ki - -
CHEMBL169 URSOLIC ACID Ki - -