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Assay Detail

CHEMBL2175863

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

Binding
Inhibition of bovine PDE4 using [3H]cAMP as substrate
33
Total Activities
33
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 33 6.41 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2172710 1 7.30
CHEMBL2172734 1 6.98
CHEMBL2172732 1 6.96
CHEMBL2172731 1 6.85
CHEMBL2172733 1 6.82
CHEMBL2172712 1 6.72
CHEMBL2172709 1 6.68
CHEMBL2172708 1 6.54
CHEMBL2172720 1 6.52
CHEMBL63 ROLIPRAM 2.0 1 6.10
CHEMBL2172713 1 5.39
CHEMBL2172714 1 5.28
CHEMBL2172715 1 5.14
CHEMBL2172727 1 -
CHEMBL2172726 1 -
CHEMBL2172725 1 -
CHEMBL2172724 1 -
CHEMBL2172723 1 -
CHEMBL2172722 1 -
CHEMBL2172730 1 -
CHEMBL2172711 1 -
CHEMBL2172719 1 -
CHEMBL2172718 1 -
CHEMBL2172717 1 -
CHEMBL538930 1 -
CHEMBL2172716 1 -
CHEMBL2172736 1 -
CHEMBL551629 1 -
CHEMBL2172735 1 -
CHEMBL2172721 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2172710 IC50 = 50.0 nM 7.30
CHEMBL2172734 IC50 = 105.0 nM 6.98
CHEMBL2172732 IC50 = 110.0 nM 6.96
CHEMBL2172731 IC50 = 140.0 nM 6.85
CHEMBL2172733 IC50 = 150.0 nM 6.82
CHEMBL2172712 IC50 = 190.0 nM 6.72
CHEMBL2172709 IC50 = 210.0 nM 6.68
CHEMBL2172708 IC50 = 290.0 nM 6.54
CHEMBL2172720 IC50 = 300.0 nM 6.52
CHEMBL63 ROLIPRAM IC50 = 800.0 nM 6.10
CHEMBL2172713 IC50 = 4100.0 nM 5.39
CHEMBL2172714 IC50 = 5200.0 nM 5.28
CHEMBL2172715 IC50 = 7300.0 nM 5.14
CHEMBL2172729 IC50 - -
CHEMBL2172728 IC50 - -
CHEMBL541778 IC50 - -
CHEMBL2172727 IC50 - -
CHEMBL2172726 IC50 - -
CHEMBL2172725 IC50 - -
CHEMBL2172724 IC50 - -
CHEMBL2172723 IC50 - -
CHEMBL2172722 IC50 - -
CHEMBL2172730 IC50 - -
CHEMBL2172711 IC50 - -
CHEMBL2172719 IC50 - -
CHEMBL2172718 IC50 - -
CHEMBL2172717 IC50 - -
CHEMBL538930 IC50 - -
CHEMBL2172716 IC50 - -
CHEMBL2172736 IC50 - -
CHEMBL551629 IC50 - -
CHEMBL2172735 IC50 - -
CHEMBL2172721 IC50 - -