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Assay Detail

CHEMBL1806340

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

Binding
Inhibition of PTP1B expressed in Escherichia coli assessed as p-nitrophenol release from pNPP substrate preincubated for 10 mins
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Novel thiazolidinedione derivatives with anti-obesity effects: dual action as PTP1B inhibitors and PPAR-γ activators.
Bhattarai BR, Kafle B, Hwang JS, Ham SW, Lee KH, Park H, Han IO, Cho H.
Bioorg Med Chem Lett (2010) 20 : 6758 -6763
PubMed 20850970 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 5.16 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1801440 1 5.89
CHEMBL1801411 1 5.85
CHEMBL1801439 1 5.70
CHEMBL1801434 1 5.64
CHEMBL1801404 1 5.40
CHEMBL1801407 1 5.40
CHEMBL1801435 1 5.22
CHEMBL1801409 1 5.22
CHEMBL1801402 1 5.10
CHEMBL1801406 1 5.05
CHEMBL1801405 1 5.05
CHEMBL1801401 1 5.05
CHEMBL1801400 1 5.00
CHEMBL1801437 1 4.96
CHEMBL1801432 1 4.92
CHEMBL1801433 1 4.92
CHEMBL1801438 1 4.85
CHEMBL1801403 1 4.80
CHEMBL1801410 1 4.72
CHEMBL1801436 1 4.48
CHEMBL1801408 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1801440 IC50 = 1300.0 nM 5.89
CHEMBL1801411 IC50 = 1400.0 nM 5.85
CHEMBL1801439 IC50 = 2000.0 nM 5.70
CHEMBL1801434 IC50 = 2300.0 nM 5.64
CHEMBL1801404 IC50 = 4000.0 nM 5.40
CHEMBL1801407 IC50 = 4000.0 nM 5.40
CHEMBL1801435 IC50 = 6000.0 nM 5.22
CHEMBL1801409 IC50 = 6000.0 nM 5.22
CHEMBL1801402 IC50 = 8000.0 nM 5.10
CHEMBL1801406 IC50 = 9000.0 nM 5.05
CHEMBL1801405 IC50 = 9000.0 nM 5.05
CHEMBL1801401 IC50 = 9000.0 nM 5.05
CHEMBL1801400 IC50 = 10000.0 nM 5.00
CHEMBL1801437 IC50 = 11000.0 nM 4.96
CHEMBL1801432 IC50 = 12000.0 nM 4.92
CHEMBL1801433 IC50 = 12000.0 nM 4.92
CHEMBL1801438 IC50 = 14000.0 nM 4.85
CHEMBL1801403 IC50 = 16000.0 nM 4.80
CHEMBL1801410 IC50 = 19000.0 nM 4.72
CHEMBL1801436 IC50 = 33000.0 nM 4.48
CHEMBL1801408 IC50 = 136000.0 nM -