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Assay Detail

CHEMBL823523

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

Functional
Compound was tested for its ability to inhibit calcium influx in human U937 cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type U-937
Confidence 1 — Organism
Curated By Intermediate

Target

Homo sapiens (CHEMBL372)
Type ORGANISM
Organism Homo sapiens

Publication

Development of 2,2-dimethylchromanol cysteinyl LT1 receptor antagonists.
Chambers RJ, Antognoli GW, Cheng JB, Kuperman AV, Liston TC, Marfat A, Owens BS, Pillar JS, Shirley JT, Watson JW.
Bioorg Med Chem Lett (1998) 8 : 3577 -3582
PubMed 9934474 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.62 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL331884 1 9.70
CHEMBL332680 1 9.52
CHEMBL119214 1 9.30
CHEMBL21333 PRANLUKAST 4.0 1 9.00
CHEMBL603 ZAFIRLUKAST 4.0 1 9.00
CHEMBL331747 1 8.70
CHEMBL300701 1 8.10
CHEMBL120200 1 7.77
CHEMBL442150 1 6.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL331884 IC50 = 0.2 nM 9.70
CHEMBL332680 IC50 = 0.3 nM 9.52
CHEMBL119214 IC50 = 0.5 nM 9.30
CHEMBL21333 PRANLUKAST IC50 = 1.0 nM 9.00
CHEMBL603 ZAFIRLUKAST IC50 = 1.0 nM 9.00
CHEMBL331747 IC50 = 2.0 nM 8.70
CHEMBL300701 IC50 = 8.0 nM 8.10
CHEMBL120200 IC50 = 17.0 nM 7.77
CHEMBL442150 IC50 = 310.0 nM 6.51