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Assay Detail

CHEMBL1114702

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

Functional
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha production by PLAP reporter assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type THP-1
Confidence 1 — Organism
Curated By Autocuration

Target

THP-1 (CHEMBL614245)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of anti-inflammatory clinical candidate E6201, inspired from resorcylic lactone LL-Z1640-2, III.
Shen Y, Boivin R, Yoneda N, Du H, Schiller S, Matsushima T, Goto M, Shirota H, Gusovsky F, Lemelin C, Jiang Y, Zhang Z, Pelletier R, Ikemori-Kawada M, Kawakami Y, Inoue A, Schnaderbeck M, Wang Y.
Bioorg Med Chem Lett (2010) 20 : 3155 -3157
PubMed 20399648 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.83 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1099077 1 7.64
CHEMBL1096417 1 7.58
CHEMBL1098080 1 7.37
CHEMBL1097999 E-6201 2.0 1 7.25
CHEMBL1097699 1 7.15
CHEMBL1097700 1 7.07
CHEMBL1097280 1 6.97
CHEMBL1097698 1 6.89
CHEMBL1096741 1 6.46
CHEMBL1097653 1 6.44
CHEMBL1096740 1 6.36
CHEMBL1097413 1 5.90
CHEMBL1098081 1 5.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1099077 IC50 = 23.0 nM 7.64
CHEMBL1096417 IC50 = 26.0 nM 7.58
CHEMBL1098080 IC50 = 43.0 nM 7.37
CHEMBL1097999 E-6201 IC50 = 56.0 nM 7.25
CHEMBL1097699 IC50 = 71.0 nM 7.15
CHEMBL1097700 IC50 = 85.0 nM 7.07
CHEMBL1097280 IC50 = 108.0 nM 6.97
CHEMBL1097698 IC50 = 129.0 nM 6.89
CHEMBL1096741 IC50 = 351.0 nM 6.46
CHEMBL1097653 IC50 = 360.0 nM 6.44
CHEMBL1096740 IC50 = 437.0 nM 6.36
CHEMBL1097413 IC50 = 1251.0 nM 5.90
CHEMBL1098081 IC50 = 2066.0 nM 5.68