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Assay Detail

CHEMBL4425319

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

Binding
Inhibition of recombinant human PDE4D7 catalytic domain expressed in baculovirus infected sf9 cells using cAMP as substrate
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.
Jansen C, Kooistra AJ, Kanev GK, Leurs R, de Esch IJ, de Graaf C.
J Med Chem (2016) 59 : 7029 -7065
PubMed 26908025 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.70 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL127944 1 8.30
CHEMBL193240 ROFLUMILAST 4.0 1 8.24
CHEMBL1232082 1 7.72
CHEMBL63 ROLIPRAM 2.0 1 6.54
CHEMBL1229663 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL127944 IC50 = 5.0 nM 8.30
CHEMBL193240 ROFLUMILAST IC50 = 5.8 nM 8.24
CHEMBL1232082 IC50 = 19.0 nM 7.72
CHEMBL63 ROLIPRAM IC50 = 288.0 nM 6.54
CHEMBL1229663 IC50 < 1.0 nM -