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Assay Detail

CHEMBL5217151

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

Binding
Inhibition of N-terminal His-tagged full length mouse LMW-PTP expressed in Escherichia coli BL21(DE3) by SDS PAGE based mass spectrometry analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Structure-Based Design of Active-Site-Directed, Highly Potent, Selective, and Orally Bioavailable Low-Molecular-Weight Protein Tyrosine Phosphatase Inhibitors.
He R, Wang J, Yu ZH, Moyers JS, Michael MD, Durham TB, Cramer JW, Qian Y, Lin A, Wu L, Noinaj N, Barrett DG, Zhang ZY.
J Med Chem (2022) 65 : 13892 -13909
PubMed 36197449 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.47 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5218807 1 8.52
CHEMBL5220114 1 7.44
CHEMBL5219519 1 7.21
CHEMBL4794972 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5218807 IC50 = 3.0 nM 8.52
CHEMBL5220114 IC50 = 36.0 nM 7.44
CHEMBL5219519 IC50 = 62.0 nM 7.21
CHEMBL4794972 IC50 = 200.0 nM 6.70