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Assay Detail

CHEMBL4011234

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

Binding
Binding affinity to human TNF-alpha soluble domain assessed as decrease in complex formation with human TNFR2 extracellular domain preincubated for 1 hr followed by receptor addition measure after 2 hrs by TR-FRET assay
2
Total Activities
2
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

Structural Basis of Small-Molecule Aggregate Induced Inhibition of a Protein-Protein Interaction.
Blevitt JM, Hack MD, Herman KL, Jackson PF, Krawczuk PJ, Lebsack AD, Liu AX, Mirzadegan T, Nelen MI, Patrick AN, Steinbacher S, Milla ME, Lumb KJ.
J Med Chem (2017) 60 : 3511 -3517
PubMed 28300404 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.94 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4060030 1 5.96
CHEMBL255489 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4060030 IC50 = 1100.0 nM 5.96
CHEMBL255489 IC50 = 1200.0 nM 5.92