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Assay Detail

CHEMBL804533

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

Binding
Displacement of [3H]batrachotoxin from rat brain sodium channel
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Sodium channel alpha subunits; brain (Types I, II, III) (CHEMBL2095171)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Studies on quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides. 8.1, 2 synthesis and pharmacological evaluation of tricyclic fused quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides as potential alpha1-adrenoceptor antagonists.
Chern JW, Tao PL, Wang KC, Gutcait A, Liu SW, Yen MH, Chien SL, Rong JK.
J Med Chem (1998) 41 : 3128 -3141
PubMed 9703460 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 5.60 6.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1744044 1 6.39
CHEMBL320068 1 5.61
CHEMBL51433 1 5.43
CHEMBL106186 1 5.32
CHEMBL107084 1 5.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1744044 Ki = 404.0 nM 6.39
CHEMBL320068 Ki = 2460.0 nM 5.61
CHEMBL51433 Ki = 3680.0 nM 5.43
CHEMBL106186 Ki = 4810.0 nM 5.32
CHEMBL107084 Ki = 5380.0 nM 5.27