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Assay Detail

CHEMBL767095

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

Binding
Displacement of [3H]rolipram from mouse brain homogenates
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Phosphodiesterase 4 (CHEMBL2111373)
Type PROTEIN FAMILY
Organism Mus musculus

Publication

Biarylcarboxylic acids and -amides: inhibition of phosphodiesterase type IV versus [3H]rolipram binding activity and their relationship to emetic behavior in the ferret.
Duplantier AJ, Biggers MS, Chambers RJ, Cheng JB, Cooper K, Damon DB, Eggler JF, Kraus KG, Marfat A, Masamune H, Pillar JS, Shirley JT, Umland JP, Watson JW.
J Med Chem (1996) 39 : 120 -125
PubMed 8568798 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.31 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282934 1 8.52
CHEMBL278386 1 8.52
CHEMBL63 ROLIPRAM 2.0 1 8.40
CHEMBL280185 1 8.30
CHEMBL21964 1 8.05
CHEMBL281781 1 7.82
CHEMBL21463 1 7.82
CHEMBL21839 1 6.96
CHEMBL21305 1 6.89
CHEMBL21327 1 6.89
CHEMBL422219 1 6.49
CHEMBL280729 1 6.18
CHEMBL22461 1 5.78
CHEMBL22898 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282934 IC50 = 3.0 nM 8.52
CHEMBL278386 IC50 = 3.0 nM 8.52
CHEMBL63 ROLIPRAM IC50 = 4.0 nM 8.40
CHEMBL280185 IC50 = 5.0 nM 8.30
CHEMBL21964 IC50 = 9.0 nM 8.05
CHEMBL281781 IC50 = 15.0 nM 7.82
CHEMBL21463 IC50 = 15.0 nM 7.82
CHEMBL21839 IC50 = 111.0 nM 6.96
CHEMBL21305 IC50 = 129.0 nM 6.89
CHEMBL21327 IC50 = 130.0 nM 6.89
CHEMBL422219 IC50 = 323.0 nM 6.49
CHEMBL280729 IC50 = 653.0 nM 6.18
CHEMBL22461 IC50 = 1680.0 nM 5.78
CHEMBL22898 IC50 = 1900.0 nM 5.72