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Assay Detail

CHEMBL759930

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

Binding
Inhibitory activity against phosphodiesterase 11 (PDE11) obtained from recombinant Sf9 expression
27
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Sf9
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A (CHEMBL2717)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological activity of beta-carboline-based type-5 phosphodiesterase inhibitors.
Maw GN, Allerton CM, Gbekor E, Million WA.
Bioorg Med Chem Lett (2003) 13 : 1425 -1428
PubMed 12668004 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 7.74 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282515 2 8.85
CHEMBL284070 1 8.70
CHEMBL33518 1 8.62
CHEMBL418594 1 8.46
CHEMBL33121 1 8.38
CHEMBL285737 1 8.37
CHEMBL286309 1 8.33
CHEMBL33627 1 8.33
CHEMBL32255 1 8.26
CHEMBL34744 1 8.19
CHEMBL34276 1 8.17
CHEMBL284560 2 7.93
CHEMBL34802 1 7.66
CHEMBL33381 1 7.51
CHEMBL779 TADALAFIL 4.0 1 7.43
CHEMBL34169 1 7.41
CHEMBL33944 1 7.37
CHEMBL284627 1 7.32
CHEMBL33147 1 7.32
CHEMBL284594 1 7.28
CHEMBL284535 1 7.15
CHEMBL284059 1 7.07
CHEMBL34628 1 6.93
CHEMBL284719 1 6.02
CHEMBL284745 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282515 IC50 = 1.4 nM 8.85
CHEMBL284070 IC50 = 2.01 nM 8.70
CHEMBL282515 IC50 = 2.2 nM 8.66
CHEMBL33518 IC50 = 2.4 nM 8.62
CHEMBL418594 IC50 = 3.5 nM 8.46
CHEMBL33121 IC50 = 4.2 nM 8.38
CHEMBL285737 IC50 = 4.3 nM 8.37
CHEMBL33627 IC50 = 4.7 nM 8.33
CHEMBL286309 IC50 = 4.7 nM 8.33
CHEMBL32255 IC50 = 5.5 nM 8.26
CHEMBL34744 IC50 = 6.5 nM 8.19
CHEMBL34276 IC50 = 6.7 nM 8.17
CHEMBL284560 IC50 = 11.8 nM 7.93
CHEMBL34802 IC50 = 22.0 nM 7.66
CHEMBL33381 IC50 = 31.0 nM 7.51
CHEMBL779 TADALAFIL IC50 = 37.0 nM 7.43
CHEMBL34169 IC50 = 39.0 nM 7.41
CHEMBL33944 IC50 = 43.0 nM 7.37
CHEMBL284560 IC50 = 44.0 nM 7.36
CHEMBL33147 IC50 = 48.0 nM 7.32
CHEMBL284627 IC50 = 48.0 nM 7.32
CHEMBL284594 IC50 = 53.0 nM 7.28
CHEMBL284535 IC50 = 71.0 nM 7.15
CHEMBL284059 IC50 = 85.0 nM 7.07
CHEMBL34628 IC50 = 118.0 nM 6.93
CHEMBL284719 IC50 = 950.0 nM 6.02
CHEMBL284745 IC50 = 1000.0 nM 6.00