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Assay Detail

CHEMBL2447643

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

Functional
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-1beta release incubated for 15 mins prior to LPS-challenge measured after 24 hrs by HTRF assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

PBMC (CHEMBL613107)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery and structure-activity relationships of 6-(benzoylamino)benzoxaboroles as orally active anti-inflammatory agents.
Akama T, Dong C, Virtucio C, Freund YR, Chen D, Orr MD, Jacobs RT, Zhang YK, Hernandez V, Liu Y, Wu A, Bu W, Liu L, Jarnagin K, Plattner JJ.
Bioorg Med Chem Lett (2013) 23 : 5870 -5873
PubMed 24075731 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 5.76 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2441391 1 6.75
CHEMBL2441375 1 6.72
CHEMBL2441377 1 5.70
CHEMBL2441383 1 5.68
CHEMBL2441379 1 5.51
CHEMBL2441392 1 5.50
CHEMBL2441376 1 5.28
CHEMBL2441393 1 4.96
CHEMBL2441378 1 -
CHEMBL2441374 1 -
CHEMBL2441395 1 -
CHEMBL2441394 1 -
CHEMBL2441382 1 -
CHEMBL2441380 1 -
CHEMBL2441390 1 -
CHEMBL2441388 1 -
CHEMBL2441387 1 -
CHEMBL2440131 1 -
CHEMBL2441386 1 -
CHEMBL2441385 1 -
CHEMBL2441384 1 -
CHEMBL1761258 1 -
CHEMBL2441381 1 -
CHEMBL2441389 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2441391 IC50 = 180.0 nM 6.75
CHEMBL2441375 IC50 = 190.0 nM 6.72
CHEMBL2441377 IC50 = 2000.0 nM 5.70
CHEMBL2441383 IC50 = 2100.0 nM 5.68
CHEMBL2441379 IC50 = 3100.0 nM 5.51
CHEMBL2441392 IC50 = 3200.0 nM 5.50
CHEMBL2441376 IC50 = 5300.0 nM 5.28
CHEMBL2441393 IC50 = 11000.0 nM 4.96
CHEMBL2441378 IC50 > 100000.0 nM -
CHEMBL2441374 IC50 > 100000.0 nM -
CHEMBL2441395 IC50 > 100000.0 nM -
CHEMBL2441394 IC50 > 100000.0 nM -
CHEMBL2441382 IC50 > 10000.0 nM -
CHEMBL2441380 IC50 > 10000.0 nM -
CHEMBL2441390 IC50 > 100000.0 nM -
CHEMBL2441388 IC50 > 100000.0 nM -
CHEMBL2441387 IC50 > 100000.0 nM -
CHEMBL2440131 IC50 > 100000.0 nM -
CHEMBL2441386 IC50 > 100000.0 nM -
CHEMBL2441385 IC50 > 100000.0 nM -
CHEMBL2441384 IC50 > 10000.0 nM -
CHEMBL1761258 IC50 > 100000.0 nM -
CHEMBL2441381 IC50 > 10000.0 nM -
CHEMBL2441389 IC50 > 10000.0 nM -