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Assay Detail

CHEMBL4809912

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 preincubated for 30 mins followed by LPS addition measured after 24 hrs by immunoassay
11
Total Activities
11
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

Identification of a Series of <i>N</i>-Methylpyridine-2-carboxamides as Potent and Selective Inhibitors of the Second Bromodomain (BD2) of the Bromo and Extra Terminal Domain (BET) Proteins.
Harrison LA, Atkinson SJ, Bassil A, Chung CW, Grandi P, Gray JRJ, Levernier E, Lewis A, Lugo D, Messenger C, Michon AM, Mitchell DJ, Preston A, Prinjha RK, Rioja I, Seal JT, Taylor S, Wall ID, Watson RJ, Woolven JM, Demont EH.
J Med Chem (2021) 64 : 10742 -10771
PubMed 34232650 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.68 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4846199 1 7.00
CHEMBL4873182 1 7.00
CHEMBL4867556 1 6.90
CHEMBL4862372 1 6.80
CHEMBL4863388 1 6.70
CHEMBL4854638 1 6.70
CHEMBL4861542 1 6.60
CHEMBL4868170 1 6.60
CHEMBL4849259 1 6.50
CHEMBL4857098 1 6.50
CHEMBL4871681 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4846199 IC50 = 100.0 nM 7.00
CHEMBL4873182 IC50 = 100.0 nM 7.00
CHEMBL4867556 IC50 = 125.89 nM 6.90
CHEMBL4862372 IC50 = 158.49 nM 6.80
CHEMBL4863388 IC50 = 199.53 nM 6.70
CHEMBL4854638 IC50 = 199.53 nM 6.70
CHEMBL4861542 IC50 = 251.19 nM 6.60
CHEMBL4868170 IC50 = 251.19 nM 6.60
CHEMBL4849259 IC50 = 316.23 nM 6.50
CHEMBL4857098 IC50 = 316.23 nM 6.50
CHEMBL4871681 IC50 = 630.96 nM 6.20