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Assay Detail

CHEMBL765680

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

Binding
Inhibition of Phosphodiesterase 4 (PDE-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

8-Methoxyquinoline-5-carboxamides as PDE4 inhibitors: a potential treatment for asthma.
Buckley GM, Cooper N, Dyke HJ, Galleway FP, Gowers L, Haughan AF, Kendall HJ, Lowe C, Maxey R, Montana JG, Naylor R, Oxford J, Peake JC, Picken CL, Runcie KA, Sabin V, Sharpe A, Warneck JB.
Bioorg Med Chem Lett (2002) 12 : 1613 -1615
PubMed 12039574 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.71 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL290100 1 9.00
CHEMBL43607 1 6.96
CHEMBL43570 1 6.92
CHEMBL39058 1 6.77
CHEMBL296358 1 6.54
CHEMBL295994 1 6.32
CHEMBL288808 1 5.72
CHEMBL63 ROLIPRAM 2.0 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL290100 IC50 = 1.0 nM 9.00
CHEMBL43607 IC50 = 110.0 nM 6.96
CHEMBL43570 IC50 = 120.0 nM 6.92
CHEMBL39058 IC50 = 170.0 nM 6.77
CHEMBL296358 IC50 = 290.0 nM 6.54
CHEMBL295994 IC50 = 480.0 nM 6.32
CHEMBL288808 IC50 = 1900.0 nM 5.72
CHEMBL63 ROLIPRAM IC50 = 3500.0 nM 5.46