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Assay Detail

CHEMBL1008313

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

Functional
Inhibition of LPS-induced TNFalpha production in human whole blood preincubated for 1 hrs before LPS challenge measured after 4 hrs by ELISA
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Blood
Confidence 1 — Organism
Curated By Autocuration

Target

Blood (CHEMBL613416)
Type TISSUE
Organism Homo sapiens

Publication

Synthesis and activity of quinolinylmethyl P1' alpha-sulfone piperidine hydroxamate inhibitors of TACE.
Zhang C, Lovering F, Behnke M, Zask A, Sandanayaka V, Sun L, Zhu Y, Xu W, Zhang Y, Levin JI.
Bioorg Med Chem Lett (2009) 19 : 3445 -3448
PubMed 19464885 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 5.32 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL495831 1 5.89
CHEMBL498032 1 5.82
CHEMBL503067 1 5.72
CHEMBL495621 1 5.62
CHEMBL495795 1 5.62
CHEMBL212481 1 5.60
CHEMBL497012 1 5.60
CHEMBL496619 1 5.55
CHEMBL380049 1 5.06
CHEMBL524533 1 4.96
CHEMBL496423 1 4.85
CHEMBL236572 1 4.85
CHEMBL497838 1 4.85
CHEMBL502796 1 4.55
CHEMBL499854 1 -
CHEMBL499313 1 -
CHEMBL447275 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL495831 IC50 = 1300.0 nM 5.89
CHEMBL498032 IC50 = 1500.0 nM 5.82
CHEMBL503067 IC50 = 1900.0 nM 5.72
CHEMBL495621 IC50 = 2400.0 nM 5.62
CHEMBL495795 IC50 = 2400.0 nM 5.62
CHEMBL212481 IC50 = 2500.0 nM 5.60
CHEMBL497012 IC50 = 2500.0 nM 5.60
CHEMBL496619 IC50 = 2800.0 nM 5.55
CHEMBL380049 IC50 = 8700.0 nM 5.06
CHEMBL524533 IC50 = 11000.0 nM 4.96
CHEMBL496423 IC50 = 14000.0 nM 4.85
CHEMBL236572 IC50 = 14000.0 nM 4.85
CHEMBL497838 IC50 = 14000.0 nM 4.85
CHEMBL502796 IC50 = 28000.0 nM 4.55
CHEMBL499854 IC50 > 50000.0 nM -
CHEMBL499313 IC50 > 50000.0 nM -
CHEMBL447275 IC50 > 50000.0 nM -