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Assay Detail

CHEMBL803575

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

Functional
Displacement of [3H]rolipram from high affinity binding site (HARBS) in rat brain membrane.
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Brain
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Phosphodiesterase 4 (CHEMBL2094267)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Synthesis and biological evaluation of 2,5-dihydropyrazol.
Crespo MI, Gràcia J, Puig C, Vega A, Bou J, Beleta J, Doménech T, Ryder H, Segarra V, Palacios JM.
Bioorg Med Chem Lett (2000) 10 : 2661 -2664
PubMed 11128646 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.74 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL63 ROLIPRAM 2.0 1 8.22
CHEMBL88990 NITRAQUAZONE 2.0 1 8.00
CHEMBL327581 1 6.05
CHEMBL88527 1 6.00
CHEMBL90189 1 5.92
CHEMBL314537 1 5.82
CHEMBL91952 1 5.70
CHEMBL316449 1 5.70
CHEMBL90335 1 5.33
CHEMBL91007 1 5.30
CHEMBL88442 1 5.25
CHEMBL314088 1 5.22
CHEMBL90920 1 4.85
CHEMBL314089 1 4.46
CHEMBL92004 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL63 ROLIPRAM IC50 = 6.0 nM 8.22
CHEMBL88990 NITRAQUAZONE IC50 = 10.0 nM 8.00
CHEMBL327581 IC50 = 900.0 nM 6.05
CHEMBL88527 IC50 = 1000.0 nM 6.00
CHEMBL90189 IC50 = 1200.0 nM 5.92
CHEMBL314537 IC50 = 1500.0 nM 5.82
CHEMBL91952 IC50 = 2000.0 nM 5.70
CHEMBL316449 IC50 = 2000.0 nM 5.70
CHEMBL90335 IC50 = 4700.0 nM 5.33
CHEMBL91007 IC50 = 5000.0 nM 5.30
CHEMBL88442 IC50 = 5600.0 nM 5.25
CHEMBL314088 IC50 = 6000.0 nM 5.22
CHEMBL90920 IC50 = 14000.0 nM 4.85
CHEMBL314089 IC50 = 35000.0 nM 4.46
CHEMBL92004 IC50 = 50000.0 nM 4.30