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Assay Detail

CHEMBL763944

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

Binding
Displacement of [3H]rolipram binding to guinea pig brain membrane
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Phosphodiesterase 4 (CHEMBL2093863)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Quaternary substituted PDE4 inhibitors I: the synthesis and in vitro evaluation of a novel series of oxindoles.
Hulme C, Poli GB, Huang FC, Souness JE, Djuric SW.
Bioorg Med Chem Lett (1998) 8 : 175 -178
PubMed 9871649 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.13 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL32442 CDP840 1 7.22
CHEMBL297296 1 6.70
CHEMBL49351 1 5.62
CHEMBL300959 1 5.58
CHEMBL301351 1 5.55
CHEMBL300038 1 -
CHEMBL301366 1 -
CHEMBL52224 1 -
CHEMBL430948 1 -
CHEMBL48221 1 -
CHEMBL296824 1 -
CHEMBL300427 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL32442 CDP840 Ki = 60.0 nM 7.22
CHEMBL297296 Ki = 200.0 nM 6.70
CHEMBL49351 Ki = 2400.0 nM 5.62
CHEMBL300959 Ki = 2600.0 nM 5.58
CHEMBL301351 Ki = 2800.0 nM 5.55
CHEMBL300038 Ki > 3700.0 nM -
CHEMBL301366 Ki > 3700.0 nM -
CHEMBL52224 Ki > 3700.0 nM -
CHEMBL430948 Ki > 3700.0 nM -
CHEMBL48221 Ki > 3700.0 nM -
CHEMBL296824 Ki > 3700.0 nM -
CHEMBL300427 Ki > 3700.0 nM -