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Assay Detail

CHEMBL4189301

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

Functional
Antiinflammatory activity in human whole blood assessed as inhibition of LPS-induced MCP1 release preincubated for 30 mins followed by LPS challenge measured after 24 hrs by immunoassay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Blood
Confidence 1 — Organism
Curated By Intermediate

Target

Blood (CHEMBL613416)
Type TISSUE
Organism Homo sapiens

Publication

Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.
Law RP, Atkinson SJ, Bamborough P, Chung CW, Demont EH, Gordon LJ, Lindon M, Prinjha RK, Watson AJB, Hirst DJ.
J Med Chem (2018) 61 : 4317 -4334
PubMed 29656650 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.20 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4213809 1 6.40
CHEMBL4218735 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4213809 IC50 = 398.11 nM 6.40
CHEMBL4218735 IC50 = 1000.0 nM 6.00