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Assay Detail

CHEMBL767096

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

Binding
Inhibition of [3H]rolipram binding to Phosphodiesterase 4 (PDE IV)
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 5 — Multiple protein complex / RNA
Curated By Expert

Target

Phosphodiesterase 4 (CHEMBL2111373)
Type PROTEIN FAMILY
Organism Mus musculus

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 8 5.05 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL63 ROLIPRAM 2.0 1 8.40
CHEMBL60985 1 5.50
CHEMBL291838 1 5.34
CHEMBL61884 1 4.30
CHEMBL60007 1 4.24
CHEMBL294606 1 4.24
CHEMBL59408 1 4.21
CHEMBL60060 1 4.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL63 ROLIPRAM IC50 = 4.0 nM 8.40
CHEMBL60985 IC50 = 3200.0 nM 5.50
CHEMBL291838 IC50 = 4600.0 nM 5.34
CHEMBL61884 IC50 = 50000.0 nM 4.30
CHEMBL60007 IC50 = 58000.0 nM 4.24
CHEMBL294606 IC50 = 57000.0 nM 4.24
CHEMBL59408 IC50 = 62000.0 nM 4.21
CHEMBL60060 IC50 = 66000.0 nM 4.18