Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL860135

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

Functional
Inhibition of LPS-induced TNFalpha production in squirrel monkey whole blood
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Saimiri sciureus
Tissue Blood
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Phosphodiesterase 4 (CHEMBL2093863)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor.
Macdonald D, Mastracchio A, Perrier H, Dubé D, Gallant M, Lacombe P, Deschênes D, Roy B, Scheigetz J, Bateman K, Li C, Trimble LA, Day S, Chauret N, Nicoll-Griffith DA, Silva JM, Huang Z, Laliberté F, Liu S, Ethier D, Pon D, Muise E, Boulet L, Chan CC, Styhler A, Charleson S, Mancini J, Masson P, Claveau D, Nicholson D, Turner M, Young RN, Girard Y.
Bioorg Med Chem Lett (2005) 15 : 5241 -5246
PubMed 16168647 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.33 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL199015 1 8.30
CHEMBL372575 1 7.96
CHEMBL371037 1 7.82
CHEMBL198564 1 6.35
CHEMBL32442 CDP840 1 6.22
CHEMBL198527 1 -
CHEMBL370220 1 -
CHEMBL198432 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL199015 IC50 = 5.0 nM 8.30
CHEMBL372575 IC50 = 11.0 nM 7.96
CHEMBL371037 IC50 = 15.0 nM 7.82
CHEMBL198564 IC50 = 450.0 nM 6.35
CHEMBL32442 CDP840 IC50 = 600.0 nM 6.22
CHEMBL198527 IC50 - -
CHEMBL370220 IC50 - -
CHEMBL198432 IC50 - -