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Assay Detail

CHEMBL842220

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

Functional
Inhibition of TNF-alpha synthesis in human monocytes
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 1 — Organism
Curated By Expert

Target

Homo sapiens (CHEMBL372)
Type ORGANISM
Organism Homo sapiens

Publication

Phthalazine PDE4 inhibitors. Part 2: the synthesis and biological evaluation of 6-methoxy-1,4-disubstituted derivatives.
Napoletano M, Norcini G, Pellacini F, Marchini F, Morazzoni G, Ferlenga P, Pradella L.
Bioorg Med Chem Lett (2001) 11 : 33 -37
PubMed 11140727 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.37 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42126 PICLAMILAST 2.0 1 8.89
CHEMBL79902 1 8.52
CHEMBL79471 1 8.10
CHEMBL79535 1 8.05
CHEMBL310387 1 7.34
CHEMBL421151 1 7.21
CHEMBL81364 1 7.14
CHEMBL312375 1 7.06
CHEMBL511115 CILOMILAST 3.0 1 6.80
CHEMBL312322 1 6.78
CHEMBL70391 1 6.65
CHEMBL63 ROLIPRAM 2.0 1 6.65
CHEMBL80107 1 6.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42126 PICLAMILAST IC50 = 1.3 nM 8.89
CHEMBL79902 IC50 = 3.0 nM 8.52
CHEMBL79471 IC50 = 8.0 nM 8.10
CHEMBL79535 IC50 = 9.0 nM 8.05
CHEMBL310387 IC50 = 46.0 nM 7.34
CHEMBL421151 IC50 = 62.0 nM 7.21
CHEMBL81364 IC50 = 72.0 nM 7.14
CHEMBL312375 IC50 = 87.0 nM 7.06
CHEMBL511115 CILOMILAST IC50 = 158.0 nM 6.80
CHEMBL312322 IC50 = 166.0 nM 6.78
CHEMBL70391 IC50 = 224.0 nM 6.65
CHEMBL63 ROLIPRAM IC50 = 225.0 nM 6.65
CHEMBL80107 IC50 = 273.0 nM 6.56