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Assay Detail

CHEMBL846286

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

Binding
Inhibitory activity against recombinant phosphodiesterase 4B (PDE4B) of human mononuclear lymphocytes
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

3',5'-cyclic-AMP phosphodiesterase 4B (CHEMBL275)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of imidazol-2-one and 2-cyanoiminoimidazole derivatives: novel series of PDE4 inhibitors.
Andrés JI, Alonso JM, Díaz A, Fernández J, Iturrino L, Martínez P, Matesanz E, Freyne EJ, Deroose F, Boeckx G, Petit D, Diels G, Megens A, Somers M, Van Wauwe J, Stoppie P, Cools M, De Clerck F, Peeters D, de Chaffoy D.
Bioorg Med Chem Lett (2002) 12 : 653 -658
PubMed 11844693 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.18 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42126 PICLAMILAST 2.0 1 9.70
CHEMBL345472 1 7.72
CHEMBL2093042 1 7.72
CHEMBL346083 1 7.68
CHEMBL158977 1 7.65
CHEMBL158487 1 7.62
CHEMBL160185 1 7.61
CHEMBL160463 1 7.55
CHEMBL158644 1 7.52
CHEMBL160603 1 7.44
CHEMBL350482 1 7.41
CHEMBL345877 1 7.25
CHEMBL1788264 1 7.24
CHEMBL158616 1 7.17
CHEMBL511115 CILOMILAST 3.0 1 7.15
CHEMBL434092 1 7.07
CHEMBL345418 1 6.96
CHEMBL160144 1 6.71
CHEMBL160360 1 6.62
CHEMBL345210 1 6.56
CHEMBL346946 1 6.49
CHEMBL158431 1 6.47
CHEMBL157535 1 6.43
CHEMBL345167 1 6.40
CHEMBL352245 1 6.31
CHEMBL63 ROLIPRAM 2.0 1 6.13
CHEMBL158982 1 -
CHEMBL157812 1 -
CHEMBL349333 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42126 PICLAMILAST IC50 = 0.2 nM 9.70
CHEMBL345472 IC50 = 19.0 nM 7.72
CHEMBL2093042 IC50 = 19.0 nM 7.72
CHEMBL346083 IC50 = 21.0 nM 7.68
CHEMBL158977 IC50 = 22.4 nM 7.65
CHEMBL158487 IC50 = 24.1 nM 7.62
CHEMBL160185 IC50 = 24.3 nM 7.61
CHEMBL160463 IC50 = 28.4 nM 7.55
CHEMBL158644 IC50 = 30.0 nM 7.52
CHEMBL160603 IC50 = 36.1 nM 7.44
CHEMBL350482 IC50 = 39.2 nM 7.41
CHEMBL345877 IC50 = 56.5 nM 7.25
CHEMBL1788264 IC50 = 57.0 nM 7.24
CHEMBL158616 IC50 = 67.6 nM 7.17
CHEMBL511115 CILOMILAST IC50 = 71.0 nM 7.15
CHEMBL434092 IC50 = 85.8 nM 7.07
CHEMBL345418 IC50 = 109.6 nM 6.96
CHEMBL160144 IC50 = 196.0 nM 6.71
CHEMBL160360 IC50 = 241.0 nM 6.62
CHEMBL345210 IC50 = 277.0 nM 6.56
CHEMBL346946 IC50 = 327.0 nM 6.49
CHEMBL158431 IC50 = 341.0 nM 6.47
CHEMBL157535 IC50 = 367.0 nM 6.43
CHEMBL345167 IC50 = 399.0 nM 6.40
CHEMBL352245 IC50 = 486.0 nM 6.31
CHEMBL63 ROLIPRAM IC50 = 741.0 nM 6.13
CHEMBL158982 IC50 > 1000.0 nM -
CHEMBL157812 IC50 < 10.0 nM -
CHEMBL349333 IC50 > 1000.0 nM -