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Assay Detail

CHEMBL760825

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

Binding
Inhibition of recombinant bovine adrenal cortex Phosphodiesterase 2 (PDE2)
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Tissue Adrenal cortex
Confidence 9 — Direct single protein target
Curated By Expert

Target

cGMP-dependent 3',5'-cyclic phosphodiesterase (CHEMBL3477)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Potent tetracyclic guanine inhibitors of PDE1 and PDE5 cyclic guanosine monophosphate phosphodiesterases with oral antihypertensive activity.
Ahn HS, Bercovici A, Boykow G, Bronnenkant A, Chackalamannil S, Chow J, Cleven R, Cook J, Czarniecki M, Domalski C, Fawzi A, Green M, Gündes A, Ho G, Laudicina M, Lindo N, Ma K, Manna M, McKittrick B, Mirzai B, Nechuta T, Neustadt B, Puchalski C, Pula K, Zhang H.
J Med Chem (1997) 40 : 2196 -2210
PubMed 9216839 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.10 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68152 1 5.82
CHEMBL431377 1 5.75
CHEMBL308249 1 5.68
CHEMBL305618 1 5.51
CHEMBL70569 1 4.96
CHEMBL18745 1 4.92
CHEMBL305617 1 4.92
CHEMBL278644 1 4.47
CHEMBL305988 1 4.46
CHEMBL304161 1 4.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68152 IC50 = 1500.0 nM 5.82
CHEMBL431377 IC50 = 1800.0 nM 5.75
CHEMBL308249 IC50 = 2100.0 nM 5.68
CHEMBL305618 IC50 = 3100.0 nM 5.51
CHEMBL70569 IC50 = 10900.0 nM 4.96
CHEMBL18745 IC50 = 12000.0 nM 4.92
CHEMBL305617 IC50 = 12000.0 nM 4.92
CHEMBL278644 IC50 = 34000.0 nM 4.47
CHEMBL305988 IC50 = 35000.0 nM 4.46
CHEMBL304161 IC50 = 35000.0 nM 4.46