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Assay Detail

CHEMBL765693

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

Binding
Inhibition of Phosphodiesterase 4
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Phosphodiesterase 4 (CHEMBL2093863)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Discovery of micromolar PDE IV inhibitors that exhibit much reduced affinity for the [3H]rolipram binding site: 3-norbornyloxy-4-methoxyphenylmethylene oxindoles
Masamune H, Cheng JB, Cooper K, Eggier JF, Marfat A, Marshall SC, Shirley JT, Tickner JE, Umland JP, Vazquez E
Bioorg Med Chem Lett (1995) 5 : 1965 -1968
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.60 6.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL291838 1 6.32
CHEMBL59408 1 5.92
CHEMBL60007 1 5.47
CHEMBL63 ROLIPRAM 2.0 1 5.46
CHEMBL294606 1 5.44
CHEMBL60985 1 5.43
CHEMBL60060 1 5.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL291838 IC50 = 480.0 nM 6.32
CHEMBL59408 IC50 = 1200.0 nM 5.92
CHEMBL60007 IC50 = 3400.0 nM 5.47
CHEMBL63 ROLIPRAM IC50 = 3500.0 nM 5.46
CHEMBL294606 IC50 = 3600.0 nM 5.44
CHEMBL60985 IC50 = 3700.0 nM 5.43
CHEMBL60060 IC50 = 7100.0 nM 5.15