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Assay Detail

CHEMBL697606

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

Functional
Ability to block the release of TNF-alpha in human monocytes
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

ADMET (CHEMBL612558)
Type ADMET

Publication

Biarylcarboxamide inhibitors of phosphodiesterase IV and tumor necrosis factor-
Chambers R, Marfat A, Cheng J, Cohan V, Damon D, Duplantier A, Hibbs T, Jenkinson T, Johnson K, Kraus K, Pettipher E, Salter E, Shirley J, Umland J
Bioorg Med Chem Lett (1997) 7 : 739 -744
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.84 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL166320 1 8.05
CHEMBL162663 1 7.62
CHEMBL165158 1 7.58
CHEMBL352153 1 7.43
CHEMBL349274 1 7.10
CHEMBL351065 1 7.09
CHEMBL353349 1 6.92
CHEMBL282934 1 6.85
CHEMBL350339 1 6.75
CHEMBL161991 1 6.72
CHEMBL166306 1 6.58
CHEMBL511115 CILOMILAST 3.0 1 6.54
CHEMBL63 ROLIPRAM 2.0 1 6.51
CHEMBL280185 1 6.50
CHEMBL164067 1 6.44
CHEMBL422031 1 5.93
CHEMBL350368 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL166320 IC50 = 9.0 nM 8.05
CHEMBL162663 IC50 = 24.0 nM 7.62
CHEMBL165158 IC50 = 26.0 nM 7.58
CHEMBL352153 IC50 = 37.0 nM 7.43
CHEMBL349274 IC50 = 80.0 nM 7.10
CHEMBL351065 IC50 = 82.0 nM 7.09
CHEMBL353349 IC50 = 120.0 nM 6.92
CHEMBL282934 IC50 = 140.0 nM 6.85
CHEMBL350339 IC50 = 180.0 nM 6.75
CHEMBL161991 IC50 = 190.0 nM 6.72
CHEMBL166306 IC50 = 260.0 nM 6.58
CHEMBL511115 CILOMILAST IC50 = 290.0 nM 6.54
CHEMBL63 ROLIPRAM IC50 = 310.0 nM 6.51
CHEMBL280185 IC50 = 320.0 nM 6.50
CHEMBL164067 IC50 = 360.0 nM 6.44
CHEMBL422031 IC50 = 1170.0 nM 5.93
CHEMBL350368 IC50 = 2310.0 nM 5.64