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Assay Detail

CHEMBL4268482

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

Binding
Inhibition of full length recombinant human N-terminal GST-tagged PDE11A4 expressed in baculovirus infected sf9 cells using FAM-cyclic-3',5-AMP as substrate after 1 hr by fluorescence polarization assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.
Zheng H, Wu Y, Sun B, Cheng C, Qiao Y, Jiang Y, Zhao S, Xie Z, Tan J, Lou H.
Eur J Med Chem (2018) 158 : 767 -780
PubMed 30245400 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.83 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4292389 1 8.40
CHEMBL779 TADALAFIL 4.0 1 7.33
CHEMBL4289291 1 7.00
CHEMBL4281590 1 6.92
CHEMBL4287438 1 6.82
CHEMBL4285199 1 6.81
CHEMBL4281081 1 6.77
CHEMBL4278136 1 6.76
CHEMBL4289471 1 6.66
CHEMBL4286052 1 6.57
CHEMBL4291228 1 6.41
CHEMBL4292970 1 6.20
CHEMBL4284224 1 6.10
CHEMBL4281766 1 -
CHEMBL4277243 1 -
CHEMBL4283473 1 -
CHEMBL4280648 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4292389 IC50 = 4.0 nM 8.40
CHEMBL779 TADALAFIL IC50 = 47.0 nM 7.33
CHEMBL4289291 IC50 = 99.0 nM 7.00
CHEMBL4281590 IC50 = 119.0 nM 6.92
CHEMBL4287438 IC50 = 153.0 nM 6.82
CHEMBL4285199 IC50 = 155.0 nM 6.81
CHEMBL4281081 IC50 = 169.0 nM 6.77
CHEMBL4278136 IC50 = 173.0 nM 6.76
CHEMBL4289471 IC50 = 219.0 nM 6.66
CHEMBL4286052 IC50 = 272.0 nM 6.57
CHEMBL4291228 IC50 = 386.0 nM 6.41
CHEMBL4292970 IC50 = 634.0 nM 6.20
CHEMBL4284224 IC50 = 802.0 nM 6.10
CHEMBL4281766 IC50 > 1000.0 nM -
CHEMBL4277243 IC50 > 1000.0 nM -
CHEMBL4283473 IC50 > 1000.0 nM -
CHEMBL4280648 IC50 > 1000.0 nM -