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Assay Detail

CHEMBL2345236

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

Functional
Antiinflammatory activity in human PBMCs assessed as inhibition of LPS-induced TNFalpha release incubated for 15 mins prior to LPS challenge measured after 24 hrs by HTRF assay
28
Total Activities
28
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

Structure-activity relationships of 6-(aminomethylphenoxy)-benzoxaborole derivatives as anti-inflammatory agent.
Akama T, Virtucio C, Dong C, Kimura R, Zhang YK, Nieman JA, Sharma R, Lu X, Sales M, Singh R, Wu A, Fan XQ, Liu L, Plattner JJ, Jarnagin K, Freund YR.
Bioorg Med Chem Lett (2013) 23 : 1680 -1683
PubMed 23411072 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 6.28 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1201362 CLOBETASOL 3.0 1 8.15
CHEMBL384467 DEXAMETHASONE 4.0 1 7.77
CHEMBL2337318 1 7.39
CHEMBL2337319 1 7.08
CHEMBL2337323 1 6.38
CHEMBL1761268 1 6.12
CHEMBL10 SB-203580 1 6.00
CHEMBL2337324 1 5.80
CHEMBL1761274 1 5.36
CHEMBL2337333 1 5.23
CHEMBL1761270 1 5.04
CHEMBL2337322 1 5.00
CHEMBL2337320 1 -
CHEMBL2331615 1 -
CHEMBL2337317 1 -
CHEMBL2337316 1 -
CHEMBL2337315 1 -
CHEMBL3217028 1 -
CHEMBL2337332 1 -
CHEMBL2337331 1 -
CHEMBL2337321 1 -
CHEMBL2337329 1 -
CHEMBL2337328 1 -
CHEMBL2337327 1 -
CHEMBL1761263 1 -
CHEMBL2337326 1 -
CHEMBL2337325 1 -
CHEMBL2337330 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1201362 CLOBETASOL IC50 = 7.0 nM 8.15
CHEMBL384467 DEXAMETHASONE IC50 = 17.0 nM 7.77
CHEMBL2337318 IC50 = 41.0 nM 7.39
CHEMBL2337319 IC50 = 83.0 nM 7.08
CHEMBL2337323 IC50 = 420.0 nM 6.38
CHEMBL1761268 IC50 = 750.0 nM 6.12
CHEMBL10 SB-203580 IC50 = 1000.0 nM 6.00
CHEMBL2337324 IC50 = 1600.0 nM 5.80
CHEMBL1761274 IC50 = 4400.0 nM 5.36
CHEMBL2337333 IC50 = 5900.0 nM 5.23
CHEMBL1761270 IC50 = 9100.0 nM 5.04
CHEMBL2337322 IC50 = 10000.0 nM 5.00
CHEMBL2337320 IC50 > 10000.0 nM -
CHEMBL2331615 IC50 > 10000.0 nM -
CHEMBL2337317 IC50 > 10000.0 nM -
CHEMBL2337316 IC50 > 10000.0 nM -
CHEMBL2337315 IC50 > 10000.0 nM -
CHEMBL3217028 IC50 > 10000.0 nM -
CHEMBL2337332 IC50 > 10000.0 nM -
CHEMBL2337331 IC50 > 10000.0 nM -
CHEMBL2337321 IC50 > 10000.0 nM -
CHEMBL2337329 IC50 > 10000.0 nM -
CHEMBL2337328 IC50 > 10000.0 nM -
CHEMBL2337327 IC50 > 10000.0 nM -
CHEMBL1761263 IC50 > 10000.0 nM -
CHEMBL2337326 IC50 > 10000.0 nM -
CHEMBL2337325 IC50 > 10000.0 nM -
CHEMBL2337330 IC50 > 10000.0 nM -