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Assay Detail

CHEMBL907525

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

Functional
Inhibition of LPS-induced TNFalpha production in 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

New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site.
Moss N, Breitfelder S, Betageri R, Cirillo PF, Fadra T, Hickey ER, Kirrane T, Kroe RR, Madwed J, Nelson RM, Pargellis CA, Qian KC, Regan J, Swinamer A, Torcellini C.
Bioorg Med Chem Lett (2007) 17 : 4242 -4247
PubMed 17560108 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.17 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL381743 1 8.05
CHEMBL392248 1 7.96
CHEMBL245584 1 7.96
CHEMBL392249 1 7.85
CHEMBL103667 DORAMAPIMOD 2.0 1 7.75
CHEMBL392247 1 7.58
CHEMBL410761 1 7.50
CHEMBL394099 1 7.44
CHEMBL246176 1 7.34
CHEMBL246377 1 7.25
CHEMBL394100 1 7.25
CHEMBL246280 1 7.16
CHEMBL245583 1 6.98
CHEMBL420047 1 6.50
CHEMBL396807 1 6.41
CHEMBL246582 1 6.33
CHEMBL393890 1 5.87
CHEMBL245386 1 5.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL381743 IC50 = 9.0 nM 8.05
CHEMBL392248 IC50 = 11.0 nM 7.96
CHEMBL245584 IC50 = 11.0 nM 7.96
CHEMBL392249 IC50 = 14.0 nM 7.85
CHEMBL103667 DORAMAPIMOD IC50 = 18.0 nM 7.75
CHEMBL392247 IC50 = 26.0 nM 7.58
CHEMBL410761 IC50 = 32.0 nM 7.50
CHEMBL394099 IC50 = 36.0 nM 7.44
CHEMBL246176 IC50 = 46.0 nM 7.34
CHEMBL246377 IC50 = 56.0 nM 7.25
CHEMBL394100 IC50 = 56.0 nM 7.25
CHEMBL246280 IC50 = 70.0 nM 7.16
CHEMBL245583 IC50 = 104.0 nM 6.98
CHEMBL420047 IC50 = 320.0 nM 6.50
CHEMBL396807 IC50 = 390.0 nM 6.41
CHEMBL246582 IC50 = 470.0 nM 6.33
CHEMBL393890 IC50 = 1350.0 nM 5.87
CHEMBL245386 IC50 = 1430.0 nM 5.84