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Assay Detail

CHEMBL654581

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

Binding
Inhibition of [3H]cAMP (NEN NET-275) binding to Calcium-Independent Phosphodiesterase from rat brain.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Phosphodiesterase 4 (CHEMBL2094267)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Nicotinamide ethers: novel inhibitors of calcium-independent phosphodiesterase and [3H]rolipram binding.
Vinick FJ, Saccomano NA, Koe BK, Nielsen JA, Williams IH, Thadeio PF, Jung S, Meltz M, Johnson J, Lebel LA.
J Med Chem (1991) 34 : 86 -89
PubMed 1825116 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.66 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL171141 1 6.66
CHEMBL354430 1 6.27
CHEMBL170122 1 6.14
CHEMBL168005 1 5.85
CHEMBL171394 1 5.75
CHEMBL168418 1 5.75
CHEMBL88990 NITRAQUAZONE 2.0 1 5.72
CHEMBL352351 1 5.66
CHEMBL352655 1 5.66
CHEMBL423073 1 5.60
CHEMBL169003 1 5.54
CHEMBL169474 1 5.51
CHEMBL353878 1 5.51
CHEMBL169911 1 5.40
CHEMBL168121 1 5.19
CHEMBL169269 1 5.01
CHEMBL169676 1 5.00
CHEMBL353471 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL171141 IC50 = 220.0 nM 6.66
CHEMBL354430 IC50 = 540.0 nM 6.27
CHEMBL170122 IC50 = 730.0 nM 6.14
CHEMBL168005 IC50 = 1400.0 nM 5.85
CHEMBL171394 IC50 = 1800.0 nM 5.75
CHEMBL168418 IC50 = 1800.0 nM 5.75
CHEMBL88990 NITRAQUAZONE IC50 = 1900.0 nM 5.72
CHEMBL352351 IC50 = 2200.0 nM 5.66
CHEMBL352655 IC50 = 2200.0 nM 5.66
CHEMBL423073 IC50 = 2500.0 nM 5.60
CHEMBL169003 IC50 = 2900.0 nM 5.54
CHEMBL169474 IC50 = 3100.0 nM 5.51
CHEMBL353878 IC50 = 3100.0 nM 5.51
CHEMBL169911 IC50 = 4000.0 nM 5.40
CHEMBL168121 IC50 = 6500.0 nM 5.19
CHEMBL169269 IC50 = 9800.0 nM 5.01
CHEMBL169676 IC50 = 10000.0 nM 5.00
CHEMBL353471 IC50 > 10000.0 nM -