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Assay Detail

CHEMBL881507

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

Binding
Inhibitory concentration against protein-tyrosine phosphatase 1B by PNPP enzyme assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Structure-based design and discovery of protein tyrosine phosphatase inhibitors incorporating novel isothiazolidinone heterocyclic phosphotyrosine mimetics.
Combs AP, Yue EW, Bower M, Ala PJ, Wayland B, Douty B, Takvorian A, Polam P, Wasserman Z, Zhu W, Crawley ML, Pruitt J, Sparks R, Glass B, Modi D, McLaughlin E, Bostrom L, Li M, Galya L, Blom K, Hillman M, Gonneville L, Reid BG, Wei M, Becker-Pasha M, Klabe R, Huber R, Li Y, Hollis G, Burn TC, Wynn R, Liu P, Metcalf B.
J Med Chem (2005) 48 : 6544 -6548
PubMed 16220970 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.70 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL382311 1 6.72
CHEMBL196526 1 5.76
CHEMBL193691 1 5.52
CHEMBL373105 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL382311 IC50 = 190.0 nM 6.72
CHEMBL196526 IC50 = 1750.0 nM 5.76
CHEMBL193691 IC50 = 3000.0 nM 5.52
CHEMBL373105 IC50 = 16000.0 nM 4.80