Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL804534

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

Binding
Inhibition of [3H]- batrachotoxin binding to sodium channel in rat neocortical membrane
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
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

Synthesis and pharmacological evaluation of phenylacetamides as sodium-channel blockers.
Roufos I, Hays SJ, Dooley DJ, Schwarz RD, Campbell GW, Probert AW.
J Med Chem (1994) 37 : 268 -274
PubMed 8295214 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 6.22 7.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL30008 FLUNARIZINE 2.0 1 7.28
CHEMBL92977 1 7.19
CHEMBL92018 1 7.14
CHEMBL92870 LIDOFLAZINE 2.0 1 7.11
CHEMBL327859 1 6.96
CHEMBL92071 1 6.89
CHEMBL93436 1 6.72
CHEMBL329245 1 6.62
CHEMBL282833 1 6.58
CHEMBL330049 1 6.42
CHEMBL93634 1 6.39
CHEMBL92918 1 6.32
CHEMBL93106 1 6.00
CHEMBL313859 1 6.00
CHEMBL93838 1 5.70
CHEMBL91288 1 5.64
CHEMBL93271 1 5.16
CHEMBL94137 1 4.82
CHEMBL91929 1 4.68
CHEMBL93065 1 4.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL30008 FLUNARIZINE Ki = 53.0 nM 7.28
CHEMBL92977 Ki = 64.0 nM 7.19
CHEMBL92018 Ki = 73.0 nM 7.14
CHEMBL92870 LIDOFLAZINE Ki = 77.0 nM 7.11
CHEMBL327859 Ki = 110.0 nM 6.96
CHEMBL92071 Ki = 130.0 nM 6.89
CHEMBL93436 Ki = 190.0 nM 6.72
CHEMBL329245 Ki = 240.0 nM 6.62
CHEMBL282833 Ki = 260.0 nM 6.58
CHEMBL330049 Ki = 380.0 nM 6.42
CHEMBL93634 Ki = 410.0 nM 6.39
CHEMBL92918 Ki = 480.0 nM 6.32
CHEMBL93106 Ki = 1000.0 nM 6.00
CHEMBL313859 Ki = 1000.0 nM 6.00
CHEMBL93838 Ki = 2000.0 nM 5.70
CHEMBL91288 Ki = 2300.0 nM 5.64
CHEMBL93271 Ki = 6900.0 nM 5.16
CHEMBL94137 Ki = 15000.0 nM 4.82
CHEMBL91929 Ki = 21000.0 nM 4.68
CHEMBL93065 Ki = 21000.0 nM 4.68