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Assay Detail

CHEMBL4259631

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

Binding
Inhibition of TNFalpha (unknown origin)-induced adhesion of BCECF fluorescence-labeled human U937 cells to human HT-29 cells pretreated for 1 hr followed by BCECF fluorescence-labeled human U937 cell/TNFalpha addition and measured after 3 hrs by fluorescence 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 Autocuration

Target

Tumor necrosis factor (CHEMBL1825)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of 6-heteroarylamino-2,4,5-trimethylpyridin-3-ols as inhibitors of TNF-α-induced cell adhesion and inflammatory bowel disease.
Park SW, Banskota S, Gurung P, Jin YJ, Kang HE, Chaudhary CL, Lee SY, Jeong BS, Kim JA, Nam TG.
Medchemcomm (2018) 9 : 1305 -1310
PubMed 30151084 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.99 6.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4284433 1 6.54
CHEMBL4277438 1 6.44
CHEMBL4280147 1 6.27
CHEMBL704 MESALAMINE 4.0 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4284433 IC50 = 290.0 nM 6.54
CHEMBL4277438 IC50 = 360.0 nM 6.44
CHEMBL4280147 IC50 = 540.0 nM 6.27
CHEMBL704 MESALAMINE IC50 = 20000.0 nM 4.70