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Assay Detail

CHEMBL860120

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

Binding
Inhibitory activity against PDE4B
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

3',5'-cyclic-AMP phosphodiesterase 4B (CHEMBL275)
Type SINGLE PROTEIN
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 20 9.15 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL381681 1 10.15
CHEMBL197392 1 9.70
CHEMBL197494 1 9.52
CHEMBL196969 1 9.52
CHEMBL198674 1 9.52
CHEMBL371037 1 9.52
CHEMBL371089 1 9.52
CHEMBL197386 1 9.52
CHEMBL199015 1 9.40
CHEMBL198853 1 9.40
CHEMBL372575 1 9.30
CHEMBL198527 1 9.30
CHEMBL198732 1 8.96
CHEMBL198722 1 8.96
CHEMBL32442 CDP840 1 8.85
CHEMBL198564 1 8.74
CHEMBL198432 1 8.64
CHEMBL370220 1 8.52
CHEMBL382545 1 8.19
CHEMBL198464 1 7.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL381681 IC50 = 0.07 nM 10.15
CHEMBL197392 IC50 = 0.2 nM 9.70
CHEMBL197494 IC50 = 0.3 nM 9.52
CHEMBL196969 IC50 = 0.3 nM 9.52
CHEMBL198674 IC50 = 0.3 nM 9.52
CHEMBL371037 IC50 = 0.3 nM 9.52
CHEMBL371089 IC50 = 0.3 nM 9.52
CHEMBL197386 IC50 = 0.3 nM 9.52
CHEMBL199015 IC50 = 0.4 nM 9.40
CHEMBL198853 IC50 = 0.4 nM 9.40
CHEMBL372575 IC50 = 0.5 nM 9.30
CHEMBL198527 IC50 = 0.5 nM 9.30
CHEMBL198732 IC50 = 1.1 nM 8.96
CHEMBL198722 IC50 = 1.1 nM 8.96
CHEMBL32442 CDP840 IC50 = 1.4 nM 8.85
CHEMBL198564 IC50 = 1.8 nM 8.74
CHEMBL198432 IC50 = 2.3 nM 8.64
CHEMBL370220 IC50 = 3.0 nM 8.52
CHEMBL382545 IC50 = 6.4 nM 8.19
CHEMBL198464 IC50 = 19.0 nM 7.72