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Assay Detail

CHEMBL804526

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

Binding
Concentration required to inhibit [3H]BTX binding to Sodium channel of rat brain
18
Total Activities
18
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

2-Alkyl-4-arylimidazoles: structurally novel sodium channel modulators.
Liberatore AM, Schulz J, Pommier J, Barthelemy MA, Huchet M, Chabrier PE, Bigg D.
Bioorg Med Chem Lett (2004) 14 : 3521 -3523
PubMed 15177465 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.77 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL332257 1 8.10
CHEMBL118603 1 7.80
CHEMBL331513 1 7.72
CHEMBL117331 1 7.60
CHEMBL119139 1 7.58
CHEMBL331942 1 7.55
CHEMBL120306 1 7.52
CHEMBL334104 1 7.16
CHEMBL119494 1 7.07
CHEMBL118682 1 7.00
CHEMBL418863 1 6.84
CHEMBL118626 1 6.49
CHEMBL119103 1 6.29
CHEMBL3037819 1 5.84
CHEMBL330800 1 5.84
CHEMBL741 LAMOTRIGINE 4.0 1 4.51
CHEMBL79 LIDOCAINE 4.0 1 4.25
CHEMBL108 CARBAMAZEPINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL332257 IC50 = 8.0 nM 8.10
CHEMBL118603 IC50 = 16.0 nM 7.80
CHEMBL331513 IC50 = 19.0 nM 7.72
CHEMBL117331 IC50 = 25.0 nM 7.60
CHEMBL119139 IC50 = 26.0 nM 7.58
CHEMBL331942 IC50 = 28.0 nM 7.55
CHEMBL120306 IC50 = 30.0 nM 7.52
CHEMBL334104 IC50 = 70.0 nM 7.16
CHEMBL119494 IC50 = 86.0 nM 7.07
CHEMBL118682 IC50 = 100.0 nM 7.00
CHEMBL418863 IC50 = 146.0 nM 6.84
CHEMBL118626 IC50 = 322.0 nM 6.49
CHEMBL119103 IC50 = 518.0 nM 6.29
CHEMBL3037819 IC50 = 1460.0 nM 5.84
CHEMBL330800 IC50 = 1460.0 nM 5.84
CHEMBL741 LAMOTRIGINE IC50 = 31000.0 nM 4.51
CHEMBL79 LIDOCAINE IC50 = 56000.0 nM 4.25
CHEMBL108 CARBAMAZEPINE IC50 = 167000.0 nM -