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Assay Detail

CHEMBL702336

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

Functional
Ability to inhibit LPS-induced TNF-alpha formation in human whole blood (HWB)
17
Total Activities
14
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 2-pyridinemethanol derivatives as potent and selective phosphodiesterase-4 inhibitors.
Ducharme Y, Friesen RW, Blouin M, Côté B, Dubé D, Ethier D, Frenette R, Laliberté F, Mancini JA, Masson P, Styhler A, Young RN, Girard Y.
Bioorg Med Chem Lett (2003) 13 : 1923 -1926
PubMed 12749899 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.24 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL61191 4 6.96
CHEMBL57524 1 6.80
CHEMBL301441 1 6.52
CHEMBL57131 1 6.47
CHEMBL56330 1 6.44
CHEMBL294717 1 6.43
CHEMBL56971 1 6.34
CHEMBL56575 1 6.31
CHEMBL299931 1 6.26
CHEMBL57095 1 6.22
CHEMBL57757 1 6.11
CHEMBL417776 1 6.05
CHEMBL57767 1 5.66
CHEMBL32442 CDP840 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL61191 IC50 = 110.0 nM 6.96
CHEMBL57524 IC50 = 160.0 nM 6.80
CHEMBL61191 IC50 = 160.0 nM 6.80
CHEMBL301441 IC50 = 300.0 nM 6.52
CHEMBL57131 IC50 = 340.0 nM 6.47
CHEMBL61191 IC50 = 350.0 nM 6.46
CHEMBL56330 IC50 = 360.0 nM 6.44
CHEMBL294717 IC50 = 370.0 nM 6.43
CHEMBL56971 IC50 = 460.0 nM 6.34
CHEMBL56575 IC50 = 490.0 nM 6.31
CHEMBL299931 IC50 = 550.0 nM 6.26
CHEMBL57095 IC50 = 600.0 nM 6.22
CHEMBL57757 IC50 = 770.0 nM 6.11
CHEMBL417776 IC50 = 890.0 nM 6.05
CHEMBL57767 IC50 = 2200.0 nM 5.66
CHEMBL61191 IC50 = 3500.0 nM 5.46
CHEMBL32442 CDP840 IC50 = 16000.0 nM 4.80