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Assay Detail

CHEMBL820381

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

Functional
Effective concentration against Xenopus oocytes expressing human heart Na channel
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Oocyte
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and structure-activity relationships of 6-heterocyclic-substituted purines as inactivation modifiers of cardiac sodium channels.
Estep KG, Josef KA, Bacon ER, Carabateas PM, Rumney S, Pilling GM, Krafte DS, Volberg WA, Dillon K, Dugrenier N.
J Med Chem (1995) 38 : 2582 -2595
PubMed 7629798 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 5.91 7.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1907677 1 7.11
CHEMBL313277 1 6.54
CHEMBL87893 1 6.36
CHEMBL1907673 1 6.35
CHEMBL312861 1 6.05
CHEMBL420045 1 6.05
CHEMBL316270 1 6.04
CHEMBL315998 1 5.99
CHEMBL314661 1 5.90
CHEMBL316248 1 5.90
CHEMBL85548 1 5.80
CHEMBL87178 1 5.71
CHEMBL313247 1 5.70
CHEMBL86348 1 5.68
CHEMBL314639 1 5.64
CHEMBL313458 CARSATRIN 2.0 1 5.64
CHEMBL87286 1 5.57
CHEMBL87085 1 5.55
CHEMBL1907675 1 5.40
CHEMBL1907676 1 5.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1907677 EC50 = 78.0 nM 7.11
CHEMBL313277 EC50 = 290.0 nM 6.54
CHEMBL87893 EC50 = 433.0 nM 6.36
CHEMBL1907673 EC50 = 447.0 nM 6.35
CHEMBL312861 EC50 = 900.0 nM 6.05
CHEMBL420045 EC50 = 900.0 nM 6.05
CHEMBL316270 EC50 = 920.0 nM 6.04
CHEMBL315998 EC50 = 1030.0 nM 5.99
CHEMBL314661 EC50 = 1260.0 nM 5.90
CHEMBL316248 EC50 = 1250.0 nM 5.90
CHEMBL85548 EC50 = 1600.0 nM 5.80
CHEMBL87178 EC50 = 1950.0 nM 5.71
CHEMBL313247 EC50 = 2000.0 nM 5.70
CHEMBL86348 EC50 = 2100.0 nM 5.68
CHEMBL314639 EC50 = 2310.0 nM 5.64
CHEMBL313458 CARSATRIN EC50 = 2310.0 nM 5.64
CHEMBL87286 EC50 = 2700.0 nM 5.57
CHEMBL87085 EC50 = 2800.0 nM 5.55
CHEMBL1907675 EC50 = 3990.0 nM 5.40
CHEMBL1907676 EC50 = 7260.0 nM 5.14