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Assay Detail

CHEMBL1921285

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 after 5 hrs by ELISA method
34
Total Activities
34
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

1,7-Naphthyridine 1-oxides as novel potent and selective inhibitors of p38 mitogen activated protein kinase.
Lumeras W, Vidal L, Vidal B, Balagué C, Orellana A, Maldonado M, Domínguez M, Segarra V, Caturla F.
J Med Chem (2011) 54 : 7899 -7910
PubMed 21999461 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 7.87 9.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1916520 1 9.33
CHEMBL1916528 1 9.15
CHEMBL1738839 1 8.92
CHEMBL1916519 1 8.85
CHEMBL1916361 1 8.82
CHEMBL1916525 1 8.72
CHEMBL1916527 1 8.70
CHEMBL1916360 1 8.60
CHEMBL1916529 1 8.49
CHEMBL1916523 1 8.43
CHEMBL1916530 1 8.41
CHEMBL1916349 1 7.85
CHEMBL1916531 1 7.82
CHEMBL1916522 1 7.80
CHEMBL1916521 1 7.46
CHEMBL1916359 1 7.43
CHEMBL1916526 1 7.39
CHEMBL1916346 1 7.30
CHEMBL1916345 1 6.90
CHEMBL1916524 1 6.90
CHEMBL1916358 1 6.86
CHEMBL1916347 1 6.84
CHEMBL1916344 1 6.73
CHEMBL1916350 1 6.72
CHEMBL1916351 1 6.31
CHEMBL1916352 1 -
CHEMBL1916353 1 -
CHEMBL1916348 1 -
CHEMBL1916354 1 -
CHEMBL1916355 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1916520 IC50 = 0.47 nM 9.33
CHEMBL1916528 IC50 = 0.7 nM 9.15
CHEMBL1738839 IC50 = 1.2 nM 8.92
CHEMBL1916519 IC50 = 1.4 nM 8.85
CHEMBL1916361 IC50 = 1.5 nM 8.82
CHEMBL1916525 IC50 = 1.9 nM 8.72
CHEMBL1916527 IC50 = 2.0 nM 8.70
CHEMBL1916360 IC50 = 2.5 nM 8.60
CHEMBL1916529 IC50 = 3.2 nM 8.49
CHEMBL1916523 IC50 = 3.7 nM 8.43
CHEMBL1916530 IC50 = 3.9 nM 8.41
CHEMBL1916349 IC50 = 14.0 nM 7.85
CHEMBL1916531 IC50 = 15.0 nM 7.82
CHEMBL1916522 IC50 = 16.0 nM 7.80
CHEMBL1916521 IC50 = 35.0 nM 7.46
CHEMBL1916359 IC50 = 37.0 nM 7.43
CHEMBL1916526 IC50 = 41.0 nM 7.39
CHEMBL1916346 IC50 = 50.0 nM 7.30
CHEMBL1916345 IC50 = 125.0 nM 6.90
CHEMBL1916524 IC50 = 126.0 nM 6.90
CHEMBL1916358 IC50 = 137.0 nM 6.86
CHEMBL1916347 IC50 = 144.0 nM 6.84
CHEMBL1916344 IC50 = 187.0 nM 6.73
CHEMBL1916350 IC50 = 190.0 nM 6.72
CHEMBL1916351 IC50 = 487.0 nM 6.31
CHEMBL1916352 IC50 - -
CHEMBL1916353 IC50 - -
CHEMBL1916348 IC50 > 1000.0 nM -
CHEMBL1916354 IC50 > 1000.0 nM -
CHEMBL1916355 IC50 - -
CHEMBL1916356 IC50 - -
CHEMBL1916357 IC50 - -
CHEMBL1914478 IC50 - -
CHEMBL1916343 IC50 - -