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Assay Detail

CHEMBL4130993

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

Functional
Inhibition of TNF-alpha-induced adhesion of BCECF-labeled human U937 cells to human HT-29 cells preincubated for 1 hr followed by TNF-alpha challenge measured after 3 hrs by fluorescence microscopic method
12
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HT-29
Confidence 1 — Organism
Curated By Intermediate

Target

HT-29 (CHEMBL384)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery and structure-activity relationship studies of 2-benzylidene-2,3-dihydro-1H-inden-1-one and benzofuran-3(2H)-one derivatives as a novel class of potential therapeutics for inflammatory bowel disease.
Kadayat TM, Banskota S, Gurung P, Bist G, Thapa Magar TB, Shrestha A, Kim JA, Lee ES.
Eur J Med Chem (2017) 137 : 575 -597
PubMed 28646757 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.76 6.30
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL426110 2 6.30
CHEMBL4170979 1 6.08
CHEMBL1171578 1 6.02
CHEMBL4160838 1 5.82
CHEMBL4159694 1 5.79
CHEMBL1172319 1 5.78
CHEMBL4160761 1 5.64
CHEMBL4160536 1 5.50
CHEMBL4166435 1 5.43
CHEMBL28591 1 5.24
CHEMBL704 MESALAMINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL426110 IC50 = 500.0 nM 6.30
CHEMBL4170979 IC50 = 830.0 nM 6.08
CHEMBL1171578 IC50 = 950.0 nM 6.02
CHEMBL4160838 IC50 = 1530.0 nM 5.82
CHEMBL4159694 IC50 = 1640.0 nM 5.79
CHEMBL1172319 IC50 = 1680.0 nM 5.78
CHEMBL4160761 IC50 = 2290.0 nM 5.64
CHEMBL4160536 IC50 = 3170.0 nM 5.50
CHEMBL4166435 IC50 = 3720.0 nM 5.43
CHEMBL28591 IC50 = 5750.0 nM 5.24
CHEMBL704 MESALAMINE IC50 = 20400000.0 nM -
CHEMBL426110 Inhibition - % -