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Assay Detail

CHEMBL4836638

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

Functional
Inhibition of LPS-induced MCP1 production in human whole blood incubated for 30 mins followed by LPS stimulation and measured after 24 hrs by mesoscale assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Blood (CHEMBL613416)
Type TISSUE
Organism Homo sapiens

Publication

Optimization of a Series of 2,3-Dihydrobenzofurans as Highly Potent, Second Bromodomain (BD2)-Selective, Bromo and Extra-Terminal Domain (BET) Inhibitors.
Lucas SCC, Atkinson SJ, Chung CW, Davis R, Gordon L, Grandi P, Gray JJR, Grimes T, Phillipou A, Preston AG, Prinjha RK, Rioja I, Taylor S, Tomkinson NCO, Wall I, Watson RJ, Woolven J, Demont EH.
J Med Chem (2021) 64 : 10711 -10741
PubMed 34260229 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.15 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4869149 1 7.80
CHEMBL4851125 1 7.00
CHEMBL4850119 1 7.00
CHEMBL4848969 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4869149 IC50 = 15.85 nM 7.80
CHEMBL4851125 IC50 = 100.0 nM 7.00
CHEMBL4850119 IC50 = 100.0 nM 7.00
CHEMBL4848969 IC50 = 158.49 nM 6.80