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Assay Detail

CHEMBL2390131

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

Functional
Antiinflammatory activity in Balb/c mouse splenocytes assessed as LPS-induced TNF-alpha production after 18 to 24 hrs by AlphaLISA
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type Splenocyte
Confidence 1 — Organism
Curated By Autocuration

Publication

Identification of the fused bicyclic 4-amino-2-phenylpyrimidine derivatives as novel and potent PDE4 inhibitors.
Goto T, Shiina A, Yoshino T, Mizukami K, Hirahara K, Suzuki O, Sogawa Y, Takahashi T, Mikkaichi T, Nakao N, Takahashi M, Hasegawa M, Sasaki S.
Bioorg Med Chem Lett (2013) 23 : 3325 -3328
PubMed 23602400 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.68 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2385759 1 9.10
CHEMBL193240 ROFLUMILAST 4.0 1 8.92
CHEMBL2385757 1 8.33
CHEMBL2385758 1 8.07
CHEMBL2385753 1 8.07
CHEMBL2385755 1 8.01
CHEMBL2385756 1 7.89
CHEMBL2385761 1 7.77
CHEMBL2385760 1 7.75
CHEMBL2385754 1 7.46
CHEMBL2385573 1 7.05
CHEMBL2385559 1 6.66
CHEMBL2385749 1 6.41
CHEMBL2385563 1 6.01
CHEMBL2385751 1 -
CHEMBL2385750 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2385759 IC50 = 0.8 nM 9.10
CHEMBL193240 ROFLUMILAST IC50 = 1.2 nM 8.92
CHEMBL2385757 IC50 = 4.7 nM 8.33
CHEMBL2385758 IC50 = 8.5 nM 8.07
CHEMBL2385753 IC50 = 8.5 nM 8.07
CHEMBL2385755 IC50 = 9.8 nM 8.01
CHEMBL2385756 IC50 = 13.0 nM 7.89
CHEMBL2385761 IC50 = 17.0 nM 7.77
CHEMBL2385760 IC50 = 18.0 nM 7.75
CHEMBL2385754 IC50 = 35.0 nM 7.46
CHEMBL2385573 IC50 = 90.0 nM 7.05
CHEMBL2385559 IC50 = 220.0 nM 6.66
CHEMBL2385749 IC50 = 390.0 nM 6.41
CHEMBL2385563 IC50 = 970.0 nM 6.01
CHEMBL2385751 IC50 > 10000.0 nM -
CHEMBL2385750 IC50 > 10000.0 nM -