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Assay Detail

CHEMBL807832

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

Functional
Concentration required to inhibit the release of tumor necrosis factor -alpha (TNF-alpha) in THP-1 cellular assay.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type THP-1
Confidence 8 — Homologous single protein target
Curated By Expert

Publication

Discovery of selective hydroxamic acid inhibitors of tumor necrosis factor-alpha converting enzyme.
Holms J, Mast K, Marcotte P, Elmore I, Li J, Pease L, Glaser K, Morgan D, Michaelides M, Davidsen S.
Bioorg Med Chem Lett (2001) 11 : 2907 -2910
PubMed 11677124 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.92 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95718 1 6.85
CHEMBL318005 1 6.75
CHEMBL99283 1 6.66
CHEMBL329302 1 6.52
CHEMBL98770 1 6.40
CHEMBL318860 1 6.36
CHEMBL99103 1 6.36
CHEMBL95305 1 6.26
CHEMBL99318 1 5.54
CHEMBL329232 1 5.46
CHEMBL99120 1 5.39
CHEMBL318484 1 5.07
CHEMBL316725 1 4.82
CHEMBL421009 1 4.39
CHEMBL99547 1 -
CHEMBL98304 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95718 IC50 = 140.0 nM 6.85
CHEMBL318005 IC50 = 180.0 nM 6.75
CHEMBL99283 IC50 = 220.0 nM 6.66
CHEMBL329302 IC50 = 300.0 nM 6.52
CHEMBL98770 IC50 = 400.0 nM 6.40
CHEMBL318860 IC50 = 440.0 nM 6.36
CHEMBL99103 IC50 = 440.0 nM 6.36
CHEMBL95305 IC50 = 550.0 nM 6.26
CHEMBL99318 IC50 = 2900.0 nM 5.54
CHEMBL329232 IC50 = 3500.0 nM 5.46
CHEMBL99120 IC50 = 4100.0 nM 5.39
CHEMBL318484 IC50 = 8600.0 nM 5.07
CHEMBL316725 IC50 = 15000.0 nM 4.82
CHEMBL421009 IC50 = 41000.0 nM 4.39
CHEMBL99547 IC50 > 5000.0 nM -
CHEMBL98304 IC50 > 5000.0 nM -