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Assay Detail

CHEMBL701318

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

Functional
Inhibition of LPS-induced TNF-alpha formation in human whole blood.
18
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Homo sapiens (CHEMBL372)
Type ORGANISM
Organism Homo sapiens

Publication

Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
Frenette R, Blouin M, Brideau C, Chauret N, Ducharme Y, Friesen RW, Hamel P, Jones TR, Laliberté F, Li C, Masson P, McAuliffe M, Girard Y.
Bioorg Med Chem Lett (2002) 12 : 3009 -3013
PubMed 12270195 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.57 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL323312 5 6.52
CHEMBL105164 1 6.52
CHEMBL286224 1 6.16
CHEMBL103635 1 6.00
CHEMBL408345 1 5.54
CHEMBL103859 1 5.41
CHEMBL318108 1 5.24
CHEMBL102718 1 5.11
CHEMBL102784 2 5.11
CHEMBL105243 1 5.10
CHEMBL319858 1 4.89
CHEMBL32442 CDP840 1 4.82
CHEMBL511115 CILOMILAST 3.0 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL323312 IC50 = 300.0 nM 6.52
CHEMBL105164 IC50 = 300.0 nM 6.52
CHEMBL323312 IC50 = 400.0 nM 6.40
CHEMBL323312 IC50 = 400.0 nM 6.40
CHEMBL286224 IC50 = 700.0 nM 6.16
CHEMBL323312 IC50 = 700.0 nM 6.16
CHEMBL103635 IC50 = 1000.0 nM 6.00
CHEMBL408345 IC50 = 2900.0 nM 5.54
CHEMBL323312 IC50 = 3700.0 nM 5.43
CHEMBL103859 IC50 = 3900.0 nM 5.41
CHEMBL318108 IC50 = 5800.0 nM 5.24
CHEMBL102718 IC50 = 7800.0 nM 5.11
CHEMBL102784 IC50 = 7800.0 nM 5.11
CHEMBL105243 IC50 = 7900.0 nM 5.10
CHEMBL319858 IC50 = 13000.0 nM 4.89
CHEMBL32442 CDP840 IC50 = 15000.0 nM 4.82
CHEMBL511115 CILOMILAST IC50 = 18000.0 nM 4.75
CHEMBL102784 IC50 = 23000.0 nM 4.64