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Assay Detail

CHEMBL2175736

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

Functional
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha production after 24 hrs by ELISA
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type PBMC
Confidence 1 — Organism
Curated By Autocuration

Target

PBMC (CHEMBL613107)
Type CELL-LINE
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
EC50 11 6.06 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL63 ROLIPRAM 2.0 1 6.89
CHEMBL2172710 1 6.28
CHEMBL2172732 1 6.27
CHEMBL2172733 1 5.99
CHEMBL2172720 1 5.93
CHEMBL2172708 1 5.90
CHEMBL2172712 1 5.89
CHEMBL2172734 1 5.84
CHEMBL2172709 1 5.80
CHEMBL2172731 1 5.76
CHEMBL2172713 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL63 ROLIPRAM EC50 = 130.0 nM 6.89
CHEMBL2172710 EC50 = 520.0 nM 6.28
CHEMBL2172732 EC50 = 540.0 nM 6.27
CHEMBL2172733 EC50 = 1030.0 nM 5.99
CHEMBL2172720 EC50 = 1180.0 nM 5.93
CHEMBL2172708 EC50 = 1270.0 nM 5.90
CHEMBL2172712 EC50 = 1300.0 nM 5.89
CHEMBL2172734 EC50 = 1450.0 nM 5.84
CHEMBL2172709 EC50 = 1590.0 nM 5.80
CHEMBL2172731 EC50 = 1750.0 nM 5.76
CHEMBL2172713 EC50 - -