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Assay Detail

CHEMBL834931

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

Functional
Dissociation constant for binding to inactivated state of rat brain NaIIa (rNav1.2) -B2 cell line stably expressed in HEK293 Cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type HEK293
Confidence 3 — Cell-line / Tissue
Curated By Intermediate

Target

Nucleic Acid (CHEMBL345)
Type NUCLEIC-ACID

Publication

Phenoxyphenyl pyridines as novel state-dependent, high-potency sodium channel inhibitors.
Shao B, Victory S, Ilyin VI, Goehring RR, Sun Q, Hogenkamp D, Hodges DD, Islam K, Sha D, Zhang C, Nguyen P, Robledo S, Sakellaropoulos G, Carter RB.
J Med Chem (2004) 47 : 4277 -4285
PubMed 15293999 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.13 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL188987 1 7.70
CHEMBL360599 1 7.05
CHEMBL188570 1 6.92
CHEMBL189873 1 6.82
CHEMBL186147 1 6.77
CHEMBL187228 1 6.60
CHEMBL287833 1 6.46
CHEMBL363448 1 6.44
CHEMBL186185 1 6.23
CHEMBL189086 1 5.58
CHEMBL189555 1 5.43
CHEMBL365720 1 4.87
CHEMBL741 LAMOTRIGINE 4.0 1 4.54
CHEMBL108 CARBAMAZEPINE 4.0 1 4.34
CHEMBL366331 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL188987 Ki = 20.0 nM 7.70
CHEMBL360599 Ki = 90.0 nM 7.05
CHEMBL188570 Ki = 120.0 nM 6.92
CHEMBL189873 Ki = 150.0 nM 6.82
CHEMBL186147 Ki = 170.0 nM 6.77
CHEMBL187228 Ki = 250.0 nM 6.60
CHEMBL287833 Ki = 350.0 nM 6.46
CHEMBL363448 Ki = 360.0 nM 6.44
CHEMBL186185 Ki = 590.0 nM 6.23
CHEMBL189086 Ki = 2640.0 nM 5.58
CHEMBL189555 Ki = 3750.0 nM 5.43
CHEMBL365720 Ki = 13400.0 nM 4.87
CHEMBL741 LAMOTRIGINE Ki = 29200.0 nM 4.54
CHEMBL108 CARBAMAZEPINE Ki = 46100.0 nM 4.34
CHEMBL366331 Ki = 386000.0 nM -