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Assay Detail

CHEMBL654577

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

Binding
Ability to inhibit [3H]nitrendipine binding to the calcium channel receptor(CCR) in rat cerebral cortex homogenate; Not active
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Voltage-gated L-type calcium channel (CHEMBL2095177)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Cardiovascular characterization of pyrrolo[2,1-d][1,5]benzothiazepine derivatives binding selectively to the peripheral-type benzodiazepine receptor (PBR): from dual PBR affinity and calcium antagonist activity to novel and selective calcium entry blockers.
Campiani G, Fiorini I, De Filippis MP, Ciani SM, Garofalo A, Nacci V, Giorgi G, Sega A, Botta M, Chiarini A, Budriesi R, Bruni G, Romeo MR, Manzoni C, Mennini T.
J Med Chem (1996) 39 : 2922 -2938
PubMed 8709127 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.91 5.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99871 1 5.91
CHEMBL317960 1 -
CHEMBL316826 1 -
CHEMBL416040 1 -
CHEMBL430465 1 -
CHEMBL328405 1 -
CHEMBL321126 1 -
CHEMBL98948 1 -
CHEMBL100175 1 -
CHEMBL284279 1 -
CHEMBL416214 1 -
CHEMBL101655 1 -
CHEMBL317219 1 -
CHEMBL284532 1 -
CHEMBL99182 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99871 IC50 = 1230.0 nM 5.91
CHEMBL317960 IC50 - nM -
CHEMBL316826 IC50 - nM -
CHEMBL416040 IC50 - nM -
CHEMBL430465 IC50 - nM -
CHEMBL328405 IC50 - nM -
CHEMBL321126 IC50 - nM -
CHEMBL98948 IC50 - nM -
CHEMBL100175 IC50 - nM -
CHEMBL284279 IC50 - nM -
CHEMBL416214 IC50 - nM -
CHEMBL101655 IC50 - nM -
CHEMBL317219 IC50 - nM -
CHEMBL284532 IC50 - nM -
CHEMBL99182 IC50 - nM -