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Assay Detail

CHEMBL846288

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

Binding
Inhibition of phosphodiesterase type IV (PDE4) activity
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Phosphodiesterase 4 (CHEMBL2093863)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Orally active indole N-oxide PDE4 inhibitors.
Hulme C, Mathew R, Moriarty K, Miller B, Ramanjulu M, Cox P, Souness J, Page KM, Uhl J, Travis J, Labaudiniere R, Huang F, Djuric SW.
Bioorg Med Chem Lett (1998) 8 : 3053 -3058
PubMed 9873675 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.44 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42126 PICLAMILAST 2.0 1 9.00
CHEMBL102635 1 8.39
CHEMBL101479 1 8.15
CHEMBL102741 1 8.10
CHEMBL103007 1 7.92
CHEMBL414417 1 7.85
CHEMBL323132 1 7.80
CHEMBL301201 1 7.75
CHEMBL102310 1 7.72
CHEMBL102503 1 7.70
CHEMBL323069 1 7.66
CHEMBL102758 1 7.62
CHEMBL318586 1 7.52
CHEMBL102876 1 7.42
CHEMBL262269 1 7.34
CHEMBL322837 1 7.10
CHEMBL299332 1 7.00
CHEMBL101368 1 6.58
CHEMBL63 ROLIPRAM 2.0 1 6.50
CHEMBL321760 1 6.38
CHEMBL104780 1 6.30
CHEMBL102020 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42126 PICLAMILAST IC50 = 1.0 nM 9.00
CHEMBL102635 IC50 = 4.1 nM 8.39
CHEMBL101479 IC50 = 7.0 nM 8.15
CHEMBL102741 IC50 = 8.0 nM 8.10
CHEMBL103007 IC50 = 12.0 nM 7.92
CHEMBL414417 IC50 = 14.0 nM 7.85
CHEMBL323132 IC50 = 16.0 nM 7.80
CHEMBL301201 IC50 = 18.0 nM 7.75
CHEMBL102310 IC50 = 19.0 nM 7.72
CHEMBL102503 IC50 = 20.0 nM 7.70
CHEMBL323069 IC50 = 22.0 nM 7.66
CHEMBL102758 IC50 = 24.0 nM 7.62
CHEMBL318586 IC50 = 30.0 nM 7.52
CHEMBL102876 IC50 = 38.0 nM 7.42
CHEMBL262269 IC50 = 46.0 nM 7.34
CHEMBL322837 IC50 = 80.0 nM 7.10
CHEMBL299332 IC50 = 100.0 nM 7.00
CHEMBL101368 IC50 = 260.0 nM 6.58
CHEMBL63 ROLIPRAM IC50 = 320.0 nM 6.50
CHEMBL321760 IC50 = 420.0 nM 6.38
CHEMBL104780 IC50 = 500.0 nM 6.30
CHEMBL102020 IC50 = 1400.0 nM 5.85