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Assay Detail

CHEMBL757885

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

Binding
Inhibition of PDE3 in homogenates of human blood platelets
10
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Phosphodiesterase 3 (CHEMBL2094125)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Novel selective PDE4 inhibitors. 1. Synthesis, structure-activity relationships, and molecular modeling of 4-(3,4-dimethoxyphenyl)-2H-phthalazin-1-ones and analogues.
Van der Mey M, Hatzelmann A, Van der Laan IJ, Sterk GJ, Thibaut U, Timmerman H.
J Med Chem (2001) 44 : 2511 -2522
PubMed 11472205 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.82 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85617 1 6.60
CHEMBL313842 ZARDAVERINE 2.0 1 6.20
CHEMBL84874 1 5.60
CHEMBL316413 2 5.40
CHEMBL313111 1 5.30
CHEMBL85556 1 -
CHEMBL315981 1 -
CHEMBL83484 1 -
CHEMBL84702 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85617 IC50 = 251.19 nM 6.60
CHEMBL313842 ZARDAVERINE IC50 = 630.96 nM 6.20
CHEMBL84874 IC50 = 2511.89 nM 5.60
CHEMBL316413 IC50 = 3981.07 nM 5.40
CHEMBL313111 IC50 = 5011.87 nM 5.30
CHEMBL85556 IC50 < 10000.0 nM -
CHEMBL315981 IC50 < 10000.0 nM -
CHEMBL83484 IC50 < 10000.0 nM -
CHEMBL84702 IC50 < 10000.0 nM -
CHEMBL316413 IC50 < 10000.0 nM -