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Assay Detail

CHEMBL768607

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

Binding
Inhibitory activity against phosphodiesterase 4 carried out in the cytosol of human neutrophils
28
Total Activities
28
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

Novel selective phosphodiesterase (PDE4) inhibitors. 4. Resolution, absolute configuration, and PDE4 inhibitory activity of cis-tetra- and cis-hexahydrophthalazinones.
Van der Mey M, Boss H, Couwenberg D, Hatzelmann A, Sterk GJ, Goubitz K, Schenk H, Timmerman H.
J Med Chem (2002) 45 : 2526 -2533
PubMed 12036361 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 7.25 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL313982 1 9.30
CHEMBL315565 1 9.20
CHEMBL314938 1 8.50
CHEMBL312868 1 8.30
CHEMBL87412 1 8.20
CHEMBL316016 1 8.00
CHEMBL315934 1 8.00
CHEMBL85753 1 7.80
CHEMBL86145 1 7.70
CHEMBL32442 CDP840 1 7.70
CHEMBL85895 1 7.40
CHEMBL440878 1 7.30
CHEMBL315248 1 7.30
CHEMBL63 ROLIPRAM 2.0 1 7.30
CHEMBL312666 1 7.10
CHEMBL312799 1 7.10
CHEMBL511115 CILOMILAST 3.0 1 7.00
CHEMBL313041 1 7.00
CHEMBL85424 1 6.90
CHEMBL86158 1 6.90
CHEMBL85197 1 6.80
CHEMBL83813 1 6.70
CHEMBL312212 1 6.60
CHEMBL82318 1 6.40
CHEMBL312101 1 6.10
CHEMBL81896 1 5.80
CHEMBL315264 1 5.60
CHEMBL84779 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL313982 IC50 = 0.5012 nM 9.30
CHEMBL315565 IC50 = 0.631 nM 9.20
CHEMBL314938 IC50 = 3.162 nM 8.50
CHEMBL312868 IC50 = 5.012 nM 8.30
CHEMBL87412 IC50 = 6.31 nM 8.20
CHEMBL316016 IC50 = 10.0 nM 8.00
CHEMBL315934 IC50 = 10.0 nM 8.00
CHEMBL85753 IC50 = 15.85 nM 7.80
CHEMBL86145 IC50 = 19.95 nM 7.70
CHEMBL32442 CDP840 IC50 = 19.95 nM 7.70
CHEMBL85895 IC50 = 39.81 nM 7.40
CHEMBL440878 IC50 = 50.12 nM 7.30
CHEMBL315248 IC50 = 50.12 nM 7.30
CHEMBL63 ROLIPRAM IC50 = 50.12 nM 7.30
CHEMBL312666 IC50 = 79.43 nM 7.10
CHEMBL312799 IC50 = 79.43 nM 7.10
CHEMBL511115 CILOMILAST IC50 = 100.0 nM 7.00
CHEMBL313041 IC50 = 100.0 nM 7.00
CHEMBL85424 IC50 = 125.89 nM 6.90
CHEMBL86158 IC50 = 125.89 nM 6.90
CHEMBL85197 IC50 = 158.49 nM 6.80
CHEMBL83813 IC50 = 199.53 nM 6.70
CHEMBL312212 IC50 = 251.19 nM 6.60
CHEMBL82318 IC50 = 398.11 nM 6.40
CHEMBL312101 IC50 = 794.33 nM 6.10
CHEMBL81896 IC50 = 1584.89 nM 5.80
CHEMBL315264 IC50 = 2511.89 nM 5.60
CHEMBL84779 IC50 = 7943.28 nM 5.10