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Assay Detail

CHEMBL2443692

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

Functional
Inhibition of LPS-induced TNFalpha production in Balb/c mouse splenocytes after 18 to 24 hrs by AlphaLISA assay
21
Total Activities
21
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

Target

Splenocyte (CHEMBL612422)
Type CELL-LINE
Organism Mus musculus

Publication

Synthesis and biological evaluation of 5-carbamoyl-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 (2013) 21 : 7025 -7037
PubMed 24094436 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.45 9.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2442465 1 9.68
CHEMBL193240 ROFLUMILAST 4.0 1 8.92
CHEMBL2442472 1 8.52
CHEMBL2442462 1 8.42
CHEMBL2442461 1 8.15
CHEMBL2442479 1 8.02
CHEMBL2442470 1 7.92
CHEMBL2442469 1 7.75
CHEMBL2442475 1 7.64
CHEMBL2442473 1 7.37
CHEMBL2442468 1 7.33
CHEMBL2442471 1 7.31
CHEMBL2442467 1 7.13
CHEMBL2442464 1 6.34
CHEMBL2442480 1 6.16
CHEMBL2442478 1 6.08
CHEMBL2442477 1 6.00
CHEMBL2442474 1 5.32
CHEMBL2440142 1 -
CHEMBL2442476 1 -
CHEMBL2442463 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2442465 IC50 = 0.21 nM 9.68
CHEMBL193240 ROFLUMILAST IC50 = 1.2 nM 8.92
CHEMBL2442472 IC50 = 3.0 nM 8.52
CHEMBL2442462 IC50 = 3.8 nM 8.42
CHEMBL2442461 IC50 = 7.1 nM 8.15
CHEMBL2442479 IC50 = 9.6 nM 8.02
CHEMBL2442470 IC50 = 12.0 nM 7.92
CHEMBL2442469 IC50 = 18.0 nM 7.75
CHEMBL2442475 IC50 = 23.0 nM 7.64
CHEMBL2442473 IC50 = 43.0 nM 7.37
CHEMBL2442468 IC50 = 47.0 nM 7.33
CHEMBL2442471 IC50 = 49.0 nM 7.31
CHEMBL2442467 IC50 = 74.0 nM 7.13
CHEMBL2442464 IC50 = 460.0 nM 6.34
CHEMBL2442480 IC50 = 690.0 nM 6.16
CHEMBL2442478 IC50 = 840.0 nM 6.08
CHEMBL2442477 IC50 = 1000.0 nM 6.00
CHEMBL2442474 IC50 = 4800.0 nM 5.32
CHEMBL2440142 IC50 - -
CHEMBL2442476 IC50 - -
CHEMBL2442463 IC50 - -