Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4222142

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

Binding
Inhibition of PDE2 (unknown origin)
18
Total Activities
18
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

cGMP-dependent 3',5'-cyclic phosphodiesterase (CHEMBL2652)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Indole acids as a novel PDE2 inhibitor chemotype that demonstrate pro-cognitive activity in multiple species.
Stachel SJ, Egbertson MS, Wai J, Machacek M, Toolan DM, Swestock J, Eddins DM, Puri V, McGaughey G, Su HP, Perlow D, Wang D, Ma L, Parthasarathy G, Reid JC, Abeywickrema PD, Smith SM, Uslaner JM.
Bioorg Med Chem Lett (2018) 28 : 1122 -1126
PubMed 29534798 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.46 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4228478 1 8.30
CHEMBL4229054 1 8.15
CHEMBL4224708 1 7.75
CHEMBL4228792 1 7.51
CHEMBL4226404 1 7.42
CHEMBL4225707 1 7.39
CHEMBL4225177 1 7.21
CHEMBL4227300 1 6.63
CHEMBL4225978 1 6.38
CHEMBL210471 1 6.37
CHEMBL4227417 1 5.81
CHEMBL4228100 1 5.55
CHEMBL4227971 1 5.46
CHEMBL1289984 1 5.31
CHEMBL4225398 1 5.21
CHEMBL4225728 1 5.18
CHEMBL4226493 1 4.17
CHEMBL4228423 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4228478 IC50 = 5.0 nM 8.30
CHEMBL4229054 IC50 = 7.0 nM 8.15
CHEMBL4224708 IC50 = 18.0 nM 7.75
CHEMBL4228792 IC50 = 31.0 nM 7.51
CHEMBL4226404 IC50 = 38.0 nM 7.42
CHEMBL4225707 IC50 = 41.0 nM 7.39
CHEMBL4225177 IC50 = 61.0 nM 7.21
CHEMBL4227300 IC50 = 233.0 nM 6.63
CHEMBL4225978 IC50 = 422.0 nM 6.38
CHEMBL210471 IC50 = 431.0 nM 6.37
CHEMBL4227417 IC50 = 1548.0 nM 5.81
CHEMBL4228100 IC50 = 2801.0 nM 5.55
CHEMBL4227971 IC50 = 3465.0 nM 5.46
CHEMBL1289984 IC50 = 4850.0 nM 5.31
CHEMBL4225398 IC50 = 6100.0 nM 5.21
CHEMBL4225728 IC50 = 6526.0 nM 5.18
CHEMBL4226493 IC50 = 66879.0 nM 4.17
CHEMBL4228423 IC50 > 278000.0 nM -