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Assay Detail

CHEMBL1042420

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

Functional
Antiinflammatory activity against Sprague-Dawley rat whole blood assessed as suppression of LPS-induced TNFalpha production by ELISA
19
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Blood
Confidence 1 — Organism
Curated By Autocuration

Target

Blood (CHEMBL613615)
Type TISSUE
Organism Rattus norvegicus

Publication

Synthesis and biological evaluation of novel phthalazinone derivatives as topically active phosphodiesterase 4 inhibitors.
Kagayama K, Morimoto T, Nagata S, Katoh F, Zhang X, Inoue N, Hashino A, Kageyama K, Shikaura J, Niwa T.
Bioorg Med Chem (2009) 17 : 6959 -6970
PubMed 19744860 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.96 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL594109 1 9.30
CHEMBL594108 1 9.15
CHEMBL596447 1 9.05
CHEMBL593877 2 9.05
CHEMBL592931 1 9.00
CHEMBL595064 1 8.52
CHEMBL596394 1 8.52
CHEMBL593656 1 8.38
CHEMBL595272 1 8.34
CHEMBL595959 1 8.04
CHEMBL595038 1 7.84
CHEMBL595039 1 7.46
CHEMBL605096 1 7.35
CHEMBL603626 1 7.24
CHEMBL605935 1 6.95
CHEMBL603194 1 6.92
CHEMBL440878 1 6.68
CHEMBL592942 1 6.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL594109 IC50 = 0.5 nM 9.30
CHEMBL594108 IC50 = 0.7 nM 9.15
CHEMBL596447 IC50 = 0.9 nM 9.05
CHEMBL593877 IC50 = 0.9 nM 9.05
CHEMBL592931 IC50 = 1.0 nM 9.00
CHEMBL595064 IC50 = 3.0 nM 8.52
CHEMBL596394 IC50 = 3.0 nM 8.52
CHEMBL593656 IC50 = 4.2 nM 8.38
CHEMBL595272 IC50 = 4.6 nM 8.34
CHEMBL595959 IC50 = 9.1 nM 8.04
CHEMBL595038 IC50 = 14.5 nM 7.84
CHEMBL595039 IC50 = 34.9 nM 7.46
CHEMBL605096 IC50 = 44.8 nM 7.35
CHEMBL603626 IC50 = 57.1 nM 7.24
CHEMBL593877 IC50 = 82.2 nM 7.08
CHEMBL605935 IC50 = 112.5 nM 6.95
CHEMBL603194 IC50 = 118.8 nM 6.92
CHEMBL440878 IC50 = 207.3 nM 6.68
CHEMBL592942 IC50 = 442.4 nM 6.35