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Assay Detail

CHEMBL4223235

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

Binding
Inhibition of recombinant human Cav3.2-alpha1 expressed in HEK293T cells assessed as decrease in KCl-induced calcium mobilization measured after 600 secs post compound addition and 300 secs post KCl addition by calcium 4 dye-based FLIPR assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Synthesis and evaluation of aminobenzothiazoles as blockers of N- and T-type calcium channels.
Sairaman A, Cardoso FC, Bispat A, Lewis RJ, Duggan PJ, Tuck KL.
Bioorg Med Chem (2018) 26 : 3046 -3059
PubMed 29622412 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 4.49 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4227475 1 5.70
CHEMBL4226823 1 4.39
CHEMBL604710 Z160 2.0 1 4.35
CHEMBL4226674 1 4.27
CHEMBL4227450 1 4.19
CHEMBL4225603 1 4.02
CHEMBL4226597 1 -
CHEMBL4229218 1 -
CHEMBL4227740 1 -
CHEMBL4226078 1 -
CHEMBL4226924 1 -
CHEMBL4224756 1 -
CHEMBL4229102 1 -
CHEMBL4225354 1 -
CHEMBL4225288 1 -
CHEMBL4226136 1 -
CHEMBL4225014 1 -
CHEMBL4225787 1 -
CHEMBL4225492 1 -
CHEMBL4226327 1 -
CHEMBL4225227 1 -
CHEMBL4226080 1 -
CHEMBL4224963 1 -
CHEMBL4225815 1 -
CHEMBL4226804 1 -
CHEMBL4227653 1 -
CHEMBL4228579 1 -
CHEMBL4224809 1 -
CHEMBL4228834 1 -
CHEMBL4225757 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4227475 IC50 = 2000.0 nM 5.70
CHEMBL4226823 IC50 = 41000.0 nM 4.39
CHEMBL604710 Z160 IC50 = 45000.0 nM 4.35
CHEMBL4226674 IC50 = 54000.0 nM 4.27
CHEMBL4227450 IC50 = 64000.0 nM 4.19
CHEMBL4225603 IC50 = 95000.0 nM 4.02
CHEMBL4227740 IC50 = 112000.0 nM -
CHEMBL4224750 IC50 = 171000.0 nM -
CHEMBL4226078 IC50 = 248000.0 nM -
CHEMBL4226924 IC50 = 492000.0 nM -
CHEMBL4224756 IC50 = 165000.0 nM -
CHEMBL4229102 IC50 = 326000.0 nM -
CHEMBL4225354 IC50 = 270000.0 nM -
CHEMBL4225288 IC50 = 195000.0 nM -
CHEMBL4226136 IC50 = 288000.0 nM -
CHEMBL4225014 IC50 = 319000.0 nM -
CHEMBL4225787 IC50 = 166000.0 nM -
CHEMBL4229218 IC50 = 109000.0 nM -
CHEMBL4226597 IC50 = 328000.0 nM -
CHEMBL4225492 IC50 = 498000.0 nM -
CHEMBL4226327 IC50 = 332000.0 nM -
CHEMBL4225227 IC50 = 521000.0 nM -
CHEMBL4226080 IC50 = 212000.0 nM -
CHEMBL4224963 IC50 = 771000.0 nM -
CHEMBL4225815 IC50 = 153000.0 nM -
CHEMBL4226804 IC50 > 1000000.0 nM -
CHEMBL4227653 IC50 = 110000.0 nM -
CHEMBL4228579 IC50 = 688000.0 nM -
CHEMBL4224809 IC50 = 300000.0 nM -
CHEMBL4228834 IC50 > 1000000.0 nM -
CHEMBL4225757 IC50 = 239000.0 nM -