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Assay Detail

CHEMBL4181992

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

Binding
Inhibition of NF-kappaB (unknown origin) expressed in human A431 cells using p-NPP as substrate incubated for 48 hrs followed by substrate addition measured after 1 hr by SEAP reporter gene assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Imidazo[1,2-a]pyridines linked with thiazoles/thiophene motif through keto spacer as potential cytotoxic agents and NF-κB inhibitors.
Vasu KK, Digwal CS, Pandya AN, Pandya DH, Sharma JA, Patel S, Agarwal M.
Bioorg Med Chem Lett (2017) 27 : 5463 -5466
PubMed 29138027 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.04 5.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL186141 ANDROGRAPHOLIDE 3.0 1 5.64
CHEMBL4202872 1 5.19
CHEMBL4211571 1 5.14
CHEMBL4212097 1 5.09
CHEMBL4215065 1 5.05
CHEMBL4214832 1 4.98
CHEMBL4207217 1 4.21
CHEMBL4203396 1 -
CHEMBL4206279 1 -
CHEMBL4211161 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL186141 ANDROGRAPHOLIDE IC50 = 2300.0 nM 5.64
CHEMBL4202872 IC50 = 6500.0 nM 5.19
CHEMBL4211571 IC50 = 7300.0 nM 5.14
CHEMBL4212097 IC50 = 8200.0 nM 5.09
CHEMBL4215065 IC50 = 8900.0 nM 5.05
CHEMBL4214832 IC50 = 10500.0 nM 4.98
CHEMBL4207217 IC50 = 61200.0 nM 4.21
CHEMBL4203396 IC50 = 184580.0 nM -
CHEMBL4206279 IC50 = 187620.0 nM -
CHEMBL4211161 IC50 = 185010.0 nM -