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Assay Detail

CHEMBL4613136

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

Binding
Inhibition of PDE1C2 (147 to 531 residues) (unknown origin) using [3H]-cGMP substrate incubated for 15 mins by liquid scintillation counting method
12
Total Activities
12
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

Publication

Discovery of Novel Selective and Orally Bioavailable Phosphodiesterase-1 Inhibitors for the Efficient Treatment of Idiopathic Pulmonary Fibrosis.
Wu Y, Tian YJ, Le ML, Zhang SR, Zhang C, Huang MX, Jiang MY, Zhang B, Luo HB.
J Med Chem (2020) 63 : 7867 -7879
PubMed 32603117 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.75 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4639341 1 9.05
CHEMBL4640793 1 8.82
CHEMBL4647278 1 8.59
CHEMBL4644729 1 8.54
CHEMBL4649493 1 8.33
CHEMBL4639286 1 7.70
CHEMBL4638381 1 7.57
CHEMBL4642557 1 7.24
CHEMBL4634240 1 7.19
CHEMBL4632429 1 6.80
CHEMBL4636141 1 6.61
CHEMBL4632723 1 6.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4639341 IC50 = 0.9 nM 9.05
CHEMBL4640793 IC50 = 1.5 nM 8.82
CHEMBL4647278 IC50 = 2.6 nM 8.59
CHEMBL4644729 IC50 = 2.9 nM 8.54
CHEMBL4649493 IC50 = 4.7 nM 8.33
CHEMBL4639286 IC50 = 20.0 nM 7.70
CHEMBL4638381 IC50 = 27.0 nM 7.57
CHEMBL4642557 IC50 = 57.0 nM 7.24
CHEMBL4634240 IC50 = 65.0 nM 7.19
CHEMBL4632429 IC50 = 157.0 nM 6.80
CHEMBL4636141 IC50 = 245.0 nM 6.61
CHEMBL4632723 IC50 = 258.0 nM 6.59