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Assay Detail

CHEMBL765418

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

Binding
Optimum inhibitory concentration required to inhibit c-GMP specific phosphodiesterase 1 (PDE1) of bovine aorta
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Synthesis and evaluation of potent and selective c-GMP phosphodiesterase inhibitors.
Ho GD, Silverman L, Bercovici A, Puchalski C, Tulshian D, Xia Y, Czarniecki M, Green M, Cleven R, Zhang H, Fawzi A.
Bioorg Med Chem Lett (1999) 9 : 7 -12
PubMed 9990447 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.29 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL278254 1 8.22
CHEMBL18524 1 7.92
CHEMBL18744 1 7.85
CHEMBL18965 1 7.85
CHEMBL19157 1 7.82
CHEMBL274965 1 7.60
CHEMBL416541 1 7.60
CHEMBL19046 1 7.51
CHEMBL18817 1 7.48
CHEMBL18745 1 7.44
CHEMBL280307 1 7.22
CHEMBL18474 1 6.96
CHEMBL18964 1 6.82
CHEMBL277317 1 6.80
CHEMBL418367 1 6.53
CHEMBL275204 1 6.46
CHEMBL278644 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL278254 IC50 = 6.0 nM 8.22
CHEMBL18524 IC50 = 12.0 nM 7.92
CHEMBL18744 IC50 = 14.0 nM 7.85
CHEMBL18965 IC50 = 14.0 nM 7.85
CHEMBL19157 IC50 = 15.0 nM 7.82
CHEMBL274965 IC50 = 25.0 nM 7.60
CHEMBL416541 IC50 = 25.0 nM 7.60
CHEMBL19046 IC50 = 31.0 nM 7.51
CHEMBL18817 IC50 = 33.0 nM 7.48
CHEMBL18745 IC50 = 36.0 nM 7.44
CHEMBL280307 IC50 = 60.0 nM 7.22
CHEMBL18474 IC50 = 110.0 nM 6.96
CHEMBL18964 IC50 = 150.0 nM 6.82
CHEMBL277317 IC50 = 160.0 nM 6.80
CHEMBL418367 IC50 = 295.0 nM 6.53
CHEMBL275204 IC50 = 350.0 nM 6.46
CHEMBL278644 IC50 = 1250.0 nM 5.90