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Assay Detail

CHEMBL945136

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
3
Total Activities
3
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

Alpha,Beta-cyclic-beta-benzamido hydroxamic acids: Novel oxaspiro[4.4]nonane templates for the discovery of potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Ott GR, Asakawa N, Liu RQ, Covington MB, Qian M, Vaddi K, Newton RC, Trzaskos JM, Christ DD, Galya L, Scholz T, Marshall W, Duan JJ.
Bioorg Med Chem Lett (2008) 18 : 1288 -1292
PubMed 18234496 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.14 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL401263 1 7.62
CHEMBL401471 1 6.97
CHEMBL251994 1 6.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL401263 IC50 = 24.0 nM 7.62
CHEMBL401471 IC50 = 108.0 nM 6.97
CHEMBL251994 IC50 = 143.0 nM 6.84