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Assay Detail

CHEMBL769679

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Binding
Inhibition of Phosphodiesterase 4 from human U937 cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U-937
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Phosphodiesterase 4 (CHEMBL2093863)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Synthesis and profile of SCH351591, a novel PDE4 inhibitor.
Billah M, Cooper N, Cuss F, Davenport RJ, Dyke HJ, Egan R, Ganguly A, Gowers L, Hannah DR, Haughan AF, Kendall HJ, Lowe C, Minnicozzi M, Montana JG, Naylor R, Oxford J, Peake JC, Piwinski JJ, Runcie KA, Sabin V, Sharpe A, Shih NY, Warneck JB.
Bioorg Med Chem Lett (2002) 12 : 1621 -1623
PubMed 12039576 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.93 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42387 1 7.46
CHEMBL40200 1 7.29
CHEMBL250546 SCH-351591 1 7.22
CHEMBL607242 1 7.16
CHEMBL288195 1 6.92
CHEMBL607241 1 6.82
CHEMBL607240 1 6.62
CHEMBL42479 1 5.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42387 IC50 = 35.0 nM 7.46
CHEMBL40200 IC50 = 51.0 nM 7.29
CHEMBL250546 SCH-351591 IC50 = 60.0 nM 7.22
CHEMBL607242 IC50 = 70.0 nM 7.16
CHEMBL288195 IC50 = 120.0 nM 6.92
CHEMBL607241 IC50 = 150.0 nM 6.82
CHEMBL607240 IC50 = 240.0 nM 6.62
CHEMBL42479 IC50 = 1120.0 nM 5.95