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Assay Detail

CHEMBL3404606

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

Binding
Inhibition of human PDE4B expressed in insect cells assessed as inhibition of [3H]cAMP to [3H]AMP hydrolysis after 30 mins by scintillation counting
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

3',5'-cyclic-AMP phosphodiesterase 4B (CHEMBL275)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-(Isopropylamino)thieno[3,2-d]pyrimidin-4(3H)-one derivatives as selective phosphodiesterase 7 inhibitors with potent in vivo efficacy.
Endo Y, Kawai K, Asano T, Amano S, Asanuma Y, Sawada K, Onodera Y, Ueo N, Takahashi N, Sonoda Y, Kamei N, Irie T.
Bioorg Med Chem Lett (2015) 25 : 1910 -1914
PubMed 25866242 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 5.90 7.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3403346 1 7.34
CHEMBL3403373 1 6.85
CHEMBL3403372 1 6.70
CHEMBL3403360 1 6.70
CHEMBL3403371 1 6.42
CHEMBL3403361 1 6.38
CHEMBL3403365 1 6.36
CHEMBL3403358 1 6.28
CHEMBL3403359 1 6.26
CHEMBL3403367 1 6.25
CHEMBL3403362 1 5.96
CHEMBL3403369 1 5.85
CHEMBL3403366 1 5.82
CHEMBL3403368 1 5.72
CHEMBL3403370 1 5.64
CHEMBL3403353 1 5.32
CHEMBL3403349 1 4.96
CHEMBL3403354 1 4.92
CHEMBL3403363 1 4.85
CHEMBL3403355 1 4.62
CHEMBL3403364 1 4.60
CHEMBL3403347 1 -
CHEMBL3403352 1 -
CHEMBL3403357 1 -
CHEMBL3403351 1 -
CHEMBL3403350 1 -
CHEMBL3403356 1 -
CHEMBL3403348 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3403346 IC50 = 46.0 nM 7.34
CHEMBL3403373 IC50 = 140.0 nM 6.85
CHEMBL3403372 IC50 = 200.0 nM 6.70
CHEMBL3403360 IC50 = 200.0 nM 6.70
CHEMBL3403371 IC50 = 380.0 nM 6.42
CHEMBL3403361 IC50 = 420.0 nM 6.38
CHEMBL3403365 IC50 = 440.0 nM 6.36
CHEMBL3403358 IC50 = 520.0 nM 6.28
CHEMBL3403359 IC50 = 550.0 nM 6.26
CHEMBL3403367 IC50 = 560.0 nM 6.25
CHEMBL3403362 IC50 = 1100.0 nM 5.96
CHEMBL3403369 IC50 = 1400.0 nM 5.85
CHEMBL3403366 IC50 = 1500.0 nM 5.82
CHEMBL3403368 IC50 = 1900.0 nM 5.72
CHEMBL3403370 IC50 = 2300.0 nM 5.64
CHEMBL3403353 IC50 = 4800.0 nM 5.32
CHEMBL3403349 IC50 = 11000.0 nM 4.96
CHEMBL3403354 IC50 = 12000.0 nM 4.92
CHEMBL3403363 IC50 = 14000.0 nM 4.85
CHEMBL3403355 IC50 = 24000.0 nM 4.62
CHEMBL3403364 IC50 = 25000.0 nM 4.60
CHEMBL3403347 IC50 - -
CHEMBL3403352 IC50 - -
CHEMBL3403357 IC50 - -
CHEMBL3403351 IC50 - -
CHEMBL3403350 IC50 - -
CHEMBL3403356 IC50 - -
CHEMBL3403348 IC50 - -