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Assay Detail

CHEMBL2175745

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

Binding
Inhibition of bovine PDE3 using [3H]cAMP as substrate
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 7 5.04 5.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2172708 1 5.35
CHEMBL2172709 1 5.21
CHEMBL2172734 1 5.17
CHEMBL2172733 1 5.17
CHEMBL2172710 1 4.93
CHEMBL2172720 1 4.73
CHEMBL2172731 1 4.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2172708 IC50 = 4500.0 nM 5.35
CHEMBL2172709 IC50 = 6200.0 nM 5.21
CHEMBL2172734 IC50 = 6700.0 nM 5.17
CHEMBL2172733 IC50 = 6700.0 nM 5.17
CHEMBL2172710 IC50 = 11800.0 nM 4.93
CHEMBL2172720 IC50 = 18800.0 nM 4.73
CHEMBL2172731 IC50 = 19600.0 nM 4.71