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Assay Detail

CHEMBL3756537

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

Functional
Anti-inflammatory activity in human THP1 cells assessed as inhibition of PMA-induced IL-1beta production after 48 hrs by ELISA
15
Total Activities
15
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

Three-component, one-pot synthesis of benzo[6,7]cyclohepta[1,2-b]pyridine derivatives under catalyst free conditions and evaluation of their anti-inflammatory activity.
Sajja Y, Vulupala HR, Bantu R, Nagarapu L, Vasamsetti SB, Kotamraju S, Nanubolu JB.
Bioorg Med Chem Lett (2016) 26 : 858 -863
PubMed 26748696 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 4.96 5.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3751875 1 5.19
CHEMBL572698 1 5.16
CHEMBL3754375 1 5.09
CHEMBL3752262 1 5.07
CHEMBL3752364 1 4.76
CHEMBL527 PIROXICAM 4.0 1 4.74
CHEMBL3754105 1 4.74
CHEMBL3754044 1 -
CHEMBL3752608 1 -
CHEMBL3754356 1 -
CHEMBL3751919 1 -
CHEMBL3754400 1 -
CHEMBL3752197 1 -
CHEMBL583491 1 -
CHEMBL3753728 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3751875 IC50 = 6500.0 nM 5.19
CHEMBL572698 IC50 = 6900.0 nM 5.16
CHEMBL3754375 IC50 = 8200.0 nM 5.09
CHEMBL3752262 IC50 = 8600.0 nM 5.07
CHEMBL3752364 IC50 = 17500.0 nM 4.76
CHEMBL527 PIROXICAM IC50 = 18100.0 nM 4.74
CHEMBL3754105 IC50 = 18200.0 nM 4.74
CHEMBL3754044 IC50 > 20000.0 nM -
CHEMBL3752608 IC50 > 20000.0 nM -
CHEMBL3754356 IC50 > 20000.0 nM -
CHEMBL3751919 IC50 > 20000.0 nM -
CHEMBL3754400 IC50 > 20000.0 nM -
CHEMBL3752197 IC50 > 20000.0 nM -
CHEMBL583491 IC50 > 20000.0 nM -
CHEMBL3753728 IC50 > 20000.0 nM -