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Assay Detail

CHEMBL780514

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

Functional
Inhibition of [3H]rolipram binding to rat brain membranes.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 5 — Multiple protein complex / RNA
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 4.54 5.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL168005 1 5.18
CHEMBL88990 NITRAQUAZONE 2.0 1 4.85
CHEMBL352655 1 4.72
CHEMBL169269 1 4.66
CHEMBL423073 1 4.64
CHEMBL354430 1 4.60
CHEMBL170122 1 4.58
CHEMBL169474 1 4.58
CHEMBL171141 1 4.57
CHEMBL171394 1 4.54
CHEMBL169003 1 4.43
CHEMBL352351 1 4.37
CHEMBL168418 1 4.31
CHEMBL169911 1 4.29
CHEMBL168121 1 4.27
CHEMBL353878 1 4.00
CHEMBL353471 1 -
CHEMBL169676 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL168005 IC50 = 6600.0 nM 5.18
CHEMBL88990 NITRAQUAZONE IC50 = 14000.0 nM 4.85
CHEMBL352655 IC50 = 19000.0 nM 4.72
CHEMBL169269 IC50 = 22000.0 nM 4.66
CHEMBL423073 IC50 = 23000.0 nM 4.64
CHEMBL354430 IC50 = 25000.0 nM 4.60
CHEMBL170122 IC50 = 26000.0 nM 4.58
CHEMBL169474 IC50 = 26000.0 nM 4.58
CHEMBL171141 IC50 = 27000.0 nM 4.57
CHEMBL171394 IC50 = 29000.0 nM 4.54
CHEMBL169003 IC50 = 37000.0 nM 4.43
CHEMBL352351 IC50 = 43000.0 nM 4.37
CHEMBL168418 IC50 = 49000.0 nM 4.31
CHEMBL169911 IC50 = 51000.0 nM 4.29
CHEMBL168121 IC50 = 54000.0 nM 4.27
CHEMBL353878 IC50 = 100000.0 nM 4.00
CHEMBL353471 IC50 > 100000.0 nM -
CHEMBL169676 IC50 > 100000.0 nM -