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Assay Detail

CHEMBL2175753

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

Binding
Inhibition of human recombinant PDE4C
4
Total Activities
4
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

3',5'-cyclic-AMP phosphodiesterase 4C (CHEMBL291)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and pharmacological evaluation of N-acylhydrazones and novel conformationally constrained compounds as selective and potent orally active phosphodiesterase-4 inhibitors.
Kümmerle AE, Schmitt M, Cardozo SV, Lugnier C, Villa P, Lopes AB, Romeiro NC, Justiniano H, Martins MA, Fraga CA, Bourguignon JJ, Barreiro EJ.
J Med Chem (2012) 55 : 7525 -7545
PubMed 22891752 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.96 6.69

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2172710 1 6.69
CHEMBL2172734 1 6.30
CHEMBL2172707 1 5.43
CHEMBL63 ROLIPRAM 2.0 1 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2172710 IC50 = 206.0 nM 6.69
CHEMBL2172734 IC50 = 505.0 nM 6.30
CHEMBL2172707 IC50 = 3690.0 nM 5.43
CHEMBL63 ROLIPRAM IC50 = 3690.0 nM 5.43