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Assay Detail

CHEMBL820078

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

Functional
Effective concentration against Xenopus oocytes expressing guinea pig heart Na channel
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
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 16 6.39 7.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL313277 1 7.07
CHEMBL420045 1 7.00
CHEMBL86653 1 6.80
CHEMBL85548 1 6.80
CHEMBL86779 1 6.69
CHEMBL83511 1 6.40
CHEMBL313247 1 6.28
CHEMBL316233 1 6.24
CHEMBL86574 1 6.24
CHEMBL312932 1 6.23
CHEMBL86679 1 6.20
CHEMBL313815 1 6.10
CHEMBL85345 1 5.99
CHEMBL177786 1 5.90
CHEMBL431485 1 5.85
CHEMBL86860 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL313277 EC50 = 85.0 nM 7.07
CHEMBL420045 EC50 = 99.0 nM 7.00
CHEMBL86653 EC50 = 158.0 nM 6.80
CHEMBL85548 EC50 = 160.0 nM 6.80
CHEMBL86779 EC50 = 204.0 nM 6.69
CHEMBL83511 EC50 = 399.0 nM 6.40
CHEMBL313247 EC50 = 526.0 nM 6.28
CHEMBL316233 EC50 = 580.0 nM 6.24
CHEMBL86574 EC50 = 580.0 nM 6.24
CHEMBL312932 EC50 = 585.0 nM 6.23
CHEMBL86679 EC50 = 630.0 nM 6.20
CHEMBL313815 EC50 = 796.0 nM 6.10
CHEMBL85345 EC50 = 1035.0 nM 5.99
CHEMBL177786 EC50 = 1260.0 nM 5.90
CHEMBL431485 EC50 = 1410.0 nM 5.85
CHEMBL86860 EC50 > 3000.0 nM -