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Assay Detail

CHEMBL828298

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

Binding
Inhibition of human Phosphodiesterase 7A1 expressed in baculovirus infected Sf9 cells
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Expert

Target

High affinity 3',5'-cyclic-AMP phosphodiesterase 7A (CHEMBL3012)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 1.
Lorthiois E, Bernardelli P, Vergne F, Oliveira C, Mafroud AK, Proust E, Heuze L, Moreau F, Idrissi M, Tertre A, Bertin B, Coupe M, Wrigglesworth R, Descours A, Soulard P, Berna P.
Bioorg Med Chem Lett (2004) 14 : 4623 -4626
PubMed 15324876 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.23 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL182703 1 8.00
CHEMBL427152 1 8.00
CHEMBL185370 1 7.40
CHEMBL185360 1 7.22
CHEMBL366319 1 7.22
CHEMBL184791 1 6.92
CHEMBL185019 1 6.80
CHEMBL185814 1 6.80
CHEMBL185460 1 6.77
CHEMBL185485 1 6.68
CHEMBL363075 1 6.41
CHEMBL362141 1 6.22
CHEMBL184081 1 6.10
CHEMBL361454 1 6.08
CHEMBL184781 1 6.01
CHEMBL184888 1 5.85
CHEMBL361048 1 5.58
CHEMBL185150 1 5.57
CHEMBL185241 1 5.53
CHEMBL184877 1 5.50
CHEMBL184153 1 5.43
CHEMBL184006 1 5.32
CHEMBL185120 1 5.18
CHEMBL184085 1 5.18
CHEMBL184600 1 5.16
CHEMBL366148 1 5.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL182703 IC50 = 10.0 nM 8.00
CHEMBL427152 IC50 = 10.0 nM 8.00
CHEMBL185370 IC50 = 40.0 nM 7.40
CHEMBL185360 IC50 = 60.0 nM 7.22
CHEMBL366319 IC50 = 60.0 nM 7.22
CHEMBL184791 IC50 = 120.0 nM 6.92
CHEMBL185019 IC50 = 160.0 nM 6.80
CHEMBL185814 IC50 = 160.0 nM 6.80
CHEMBL185460 IC50 = 170.0 nM 6.77
CHEMBL185485 IC50 = 210.0 nM 6.68
CHEMBL363075 IC50 = 390.0 nM 6.41
CHEMBL362141 IC50 = 600.0 nM 6.22
CHEMBL184081 IC50 = 790.0 nM 6.10
CHEMBL361454 IC50 = 840.0 nM 6.08
CHEMBL184781 IC50 = 980.0 nM 6.01
CHEMBL184888 IC50 = 1400.0 nM 5.85
CHEMBL361048 IC50 = 2660.0 nM 5.58
CHEMBL185150 IC50 = 2700.0 nM 5.57
CHEMBL185241 IC50 = 2960.0 nM 5.53
CHEMBL184877 IC50 = 3200.0 nM 5.50
CHEMBL184153 IC50 = 3700.0 nM 5.43
CHEMBL184006 IC50 = 4800.0 nM 5.32
CHEMBL185120 IC50 = 6600.0 nM 5.18
CHEMBL184085 IC50 = 6540.0 nM 5.18
CHEMBL184600 IC50 = 6850.0 nM 5.16
CHEMBL366148 IC50 = 9500.0 nM 5.02