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Assay Detail

CHEMBL933320

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

Functional
Inhibition of LPS-induced TNFalpha production in human THP1 cells
18
Total Activities
18
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

The design and synthesis of novel alpha-ketoamide-based p38 MAP kinase inhibitors.
Montalban AG, Boman E, Chang CD, Ceide SC, Dahl R, Dalesandro D, Delaet NG, Erb E, Ernst JT, Gibbs A, Kahl J, Kessler L, Lundström J, Miller S, Nakanishi H, Roberts E, Saiah E, Sullivan R, Wang Z, Larson CJ.
Bioorg Med Chem Lett (2008) 18 : 1772 -1777
PubMed 18325768 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.41 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL103667 DORAMAPIMOD 2.0 1 7.89
CHEMBL10 SB-203580 1 7.80
CHEMBL255410 1 7.64
CHEMBL119385 NEFLAMAPIMOD 2.0 1 7.41
CHEMBL404887 1 6.66
CHEMBL255153 1 6.47
CHEMBL270617 1 6.36
CHEMBL404722 1 6.36
CHEMBL255613 1 6.36
CHEMBL270614 1 6.35
CHEMBL255972 1 6.01
CHEMBL401704 1 5.85
CHEMBL429254 1 5.82
CHEMBL270405 1 5.82
CHEMBL257519 1 5.82
CHEMBL257041 1 5.68
CHEMBL255411 1 5.58
CHEMBL401984 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL103667 DORAMAPIMOD IC50 = 13.0 nM 7.89
CHEMBL10 SB-203580 IC50 = 16.0 nM 7.80
CHEMBL255410 IC50 = 23.0 nM 7.64
CHEMBL119385 NEFLAMAPIMOD IC50 = 39.0 nM 7.41
CHEMBL404887 IC50 = 220.0 nM 6.66
CHEMBL255153 IC50 = 340.0 nM 6.47
CHEMBL270617 IC50 = 440.0 nM 6.36
CHEMBL404722 IC50 = 440.0 nM 6.36
CHEMBL255613 IC50 = 440.0 nM 6.36
CHEMBL270614 IC50 = 450.0 nM 6.35
CHEMBL255972 IC50 = 970.0 nM 6.01
CHEMBL401704 IC50 = 1400.0 nM 5.85
CHEMBL429254 IC50 = 1500.0 nM 5.82
CHEMBL270405 IC50 = 1500.0 nM 5.82
CHEMBL257519 IC50 = 1500.0 nM 5.82
CHEMBL257041 IC50 = 2100.0 nM 5.68
CHEMBL255411 IC50 = 2600.0 nM 5.58
CHEMBL401984 IC50 = 2900.0 nM 5.54