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Assay Detail

CHEMBL982653

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Binding
Inhibition of CRAC channel-mediated calcium influx in human Jurkat cells
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Jurkat
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Novel potent and selective Ca2+ release-activated Ca2+ (CRAC) channel inhibitors. Part 3: synthesis and CRAC channel inhibitory activity of 4'-[(trifluoromethyl)pyrazol-1-yl]carboxanilides.
Yonetoku Y, Kubota H, Miyazaki Y, Okamoto Y, Funatsu M, Yoshimura-Ishikawa N, Ishikawa J, Yoshino T, Takeuchi M, Ohta M.
Bioorg Med Chem (2008) 16 : 9457 -9466
PubMed 18835179 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.48 7.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL459002 1 7.11
CHEMBL484354 1 7.09
CHEMBL485208 1 7.04
CHEMBL456851 1 6.96
CHEMBL445490 1 6.92
CHEMBL262766 1 6.82
CHEMBL456852 1 6.82
CHEMBL483198 1 6.80
CHEMBL521021 1 6.68
CHEMBL456853 1 6.66
CHEMBL520993 1 6.66
CHEMBL519699 1 6.64
CHEMBL431431 1 6.62
CHEMBL485590 1 6.62
CHEMBL521340 1 6.60
CHEMBL514728 1 6.57
CHEMBL485396 1 6.54
CHEMBL485411 1 6.54
CHEMBL504268 1 6.40
CHEMBL485405 1 6.37
CHEMBL484365 1 6.34
CHEMBL484185 1 6.14
CHEMBL485241 1 6.11
CHEMBL484364 1 6.02
CHEMBL458749 1 5.80
CHEMBL485596 1 5.48
CHEMBL484363 1 4.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL459002 IC50 = 77.0 nM 7.11
CHEMBL484354 IC50 = 82.0 nM 7.09
CHEMBL485208 IC50 = 92.0 nM 7.04
CHEMBL456851 IC50 = 110.0 nM 6.96
CHEMBL445490 IC50 = 120.0 nM 6.92
CHEMBL262766 IC50 = 150.0 nM 6.82
CHEMBL456852 IC50 = 150.0 nM 6.82
CHEMBL483198 IC50 = 160.0 nM 6.80
CHEMBL521021 IC50 = 210.0 nM 6.68
CHEMBL456853 IC50 = 220.0 nM 6.66
CHEMBL520993 IC50 = 220.0 nM 6.66
CHEMBL519699 IC50 = 230.0 nM 6.64
CHEMBL431431 IC50 = 240.0 nM 6.62
CHEMBL485590 IC50 = 240.0 nM 6.62
CHEMBL521340 IC50 = 250.0 nM 6.60
CHEMBL514728 IC50 = 270.0 nM 6.57
CHEMBL485396 IC50 = 290.0 nM 6.54
CHEMBL485411 IC50 = 290.0 nM 6.54
CHEMBL504268 IC50 = 400.0 nM 6.40
CHEMBL485405 IC50 = 430.0 nM 6.37
CHEMBL484365 IC50 = 460.0 nM 6.34
CHEMBL484185 IC50 = 720.0 nM 6.14
CHEMBL485241 IC50 = 780.0 nM 6.11
CHEMBL484364 IC50 = 960.0 nM 6.02
CHEMBL458749 IC50 = 1600.0 nM 5.80
CHEMBL485596 IC50 = 3300.0 nM 5.48
CHEMBL484363 IC50 = 22000.0 nM 4.66