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Assay Detail

CHEMBL833774

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Functional
inhibitory concentration against ATP-dependant calcium influx across plasma membrane of human monocytes
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Plasma
Cell Type Cell line
Confidence 1 — Organism
Curated By Intermediate

Target

Cell line (CHEMBL614840)
Type CELL-LINE
Organism Homo sapiens

Publication

Synthesis, radiolabeling, and preliminary biological evaluation of [3H]-1-[(S)-N,O-bis-(isoquinolinesulfonyl)-N-methyl-tyrosyl]-4-(o-tolyl)-piperazine, a potent antagonist radioligand for the P2X7 receptor.
Romagnoli R, Baraldi PG, Pavani MG, Tabrizi MA, Moorman AR, Di Virgilio F, Cattabriga E, Pancaldi C, Gessi S, Borea PA.
Bioorg Med Chem Lett (2004) 14 : 5709 -5712
PubMed 15482953 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.56 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL28262 1 7.82
CHEMBL28324 1 7.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL28262 IC50 = 15.0 nM 7.82
CHEMBL28324 IC50 = 51.0 nM 7.29