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Assay Detail

CHEMBL5524536

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

Binding
Inhibition of PTPN2 in IFN-gamma induced mouse B16-F10 cells
15
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type B16-F10
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and structure-activity optimization of azepane-containing derivatives as PTPN2/PTPN1 inhibitors.
Zheng J, Zhang Z, Ding X, Sun D, Min L, Wang F, Shi S, Cai X, Zhang M, Aliper A, Ren F, Ding X, Zhavoronkov A.
Eur J Med Chem (2024) 270 : 116390 -116390
PubMed 38604096 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.31 7.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5095164 OSUNPROTAFIB 2.0 1 7.36
CHEMBL5564604 1 6.93
CHEMBL5559660 1 6.67
CHEMBL5557812 1 6.61
CHEMBL5561163 2 6.56
CHEMBL5562456 1 6.46
CHEMBL5564299 1 6.42
CHEMBL5559694 1 6.40
CHEMBL5560433 1 6.37
CHEMBL5562964 1 6.34
CHEMBL5567463 1 6.17
CHEMBL5561180 1 5.99
CHEMBL5561962 1 5.27
CHEMBL5561290 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5095164 OSUNPROTAFIB IC50 = 44.0 nM 7.36
CHEMBL5564604 IC50 = 117.0 nM 6.93
CHEMBL5559660 IC50 = 212.0 nM 6.67
CHEMBL5557812 IC50 = 247.0 nM 6.61
CHEMBL5561163 IC50 = 276.0 nM 6.56
CHEMBL5562456 IC50 = 350.0 nM 6.46
CHEMBL5564299 IC50 = 378.0 nM 6.42
CHEMBL5559694 IC50 = 399.0 nM 6.40
CHEMBL5560433 IC50 = 425.0 nM 6.37
CHEMBL5562964 IC50 = 461.0 nM 6.34
CHEMBL5561163 IC50 = 455.0 nM 6.34
CHEMBL5567463 IC50 = 669.0 nM 6.17
CHEMBL5561180 IC50 = 1033.0 nM 5.99
CHEMBL5561962 IC50 = 5332.0 nM 5.27
CHEMBL5561290 IC50 = 17739.0 nM 4.75