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Assay Detail

CHEMBL760758

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

Binding
Inhibition activity against human monocyte derived PDE4 catalytic activity (LPDE4)
19
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Phosphodiesterase 4 (CHEMBL2093863)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.
Christensen SB, Guider A, Forster CJ, Gleason JG, Bender PE, Karpinski JM, DeWolf WE, Barnette MS, Underwood DC, Griswold DE, Cieslinski LB, Burman M, Bochnowicz S, Osborn RR, Manning CD, Grous M, Hillegas LM, Bartus JO, Ryan MD, Eggleston DS, Haltiwanger RC, Torphy TJ.
J Med Chem (1998) 41 : 821 -835
PubMed 9526558 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.39 7.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL352628 1 7.36
CHEMBL354447 1 7.28
CHEMBL169537 1 7.10
CHEMBL511115 CILOMILAST 3.0 4 7.02
CHEMBL167486 1 6.92
CHEMBL167166 1 6.71
CHEMBL430893 (-)-ROLIPRAM 1 6.52
CHEMBL166529 1 6.50
CHEMBL169834 1 6.47
CHEMBL169746 1 6.30
CHEMBL352857 1 6.13
CHEMBL325795 S-ROLIPRAM 1 5.96
CHEMBL354656 1 5.93
CHEMBL167258 1 5.92
CHEMBL167638 1 5.92
CHEMBL168989 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL352628 IC50 = 44.0 nM 7.36
CHEMBL354447 IC50 = 52.0 nM 7.28
CHEMBL169537 IC50 = 80.0 nM 7.10
CHEMBL511115 CILOMILAST IC50 = 95.0 nM 7.02
CHEMBL167486 IC50 = 120.0 nM 6.92
CHEMBL167166 IC50 = 195.0 nM 6.71
CHEMBL430893 (-)-ROLIPRAM IC50 = 300.0 nM 6.52
CHEMBL166529 IC50 = 320.0 nM 6.50
CHEMBL169834 IC50 = 340.0 nM 6.47
CHEMBL169746 IC50 = 500.0 nM 6.30
CHEMBL511115 CILOMILAST IC50 = 530.0 nM 6.28
CHEMBL352857 IC50 = 740.0 nM 6.13
CHEMBL511115 CILOMILAST IC50 = 1070.0 nM 5.97
CHEMBL325795 S-ROLIPRAM IC50 = 1100.0 nM 5.96
CHEMBL354656 IC50 = 1180.0 nM 5.93
CHEMBL167638 IC50 = 1200.0 nM 5.92
CHEMBL167258 IC50 = 1200.0 nM 5.92
CHEMBL168989 IC50 = 2500.0 nM 5.60
CHEMBL511115 CILOMILAST IC50 = 3410.0 nM 5.47