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Assay Detail

CHEMBL853270

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

Toxicity
Inhibition of hERG potassium channel in HEK293 cells by patch clamp assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Toxicity
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Publication

An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression.
Becker OM, Dhanoa DS, Marantz Y, Chen D, Shacham S, Cheruku S, Heifetz A, Mohanty P, Fichman M, Sharadendu A, Nudelman R, Kauffman M, Noiman S.
J Med Chem (2006) 49 : 3116 -3135
PubMed 16722631 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.14 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296419 ASTEMIZOLE 4.0 1 9.05
CHEMBL210537 1 6.52
CHEMBL377697 1 5.82
CHEMBL211012 1 5.70
CHEMBL207478 1 5.66
CHEMBL379984 1 5.52
CHEMBL209821 NALUZOTAN 3.0 1 5.42
CHEMBL207220 1 5.40
CHEMBL209324 1 -
CHEMBL411941 CYCLORGDFV 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296419 ASTEMIZOLE IC50 = 0.9 nM 9.05
CHEMBL210537 IC50 = 300.0 nM 6.52
CHEMBL377697 IC50 = 1500.0 nM 5.82
CHEMBL211012 IC50 = 2000.0 nM 5.70
CHEMBL207478 IC50 = 2200.0 nM 5.66
CHEMBL379984 IC50 = 3000.0 nM 5.52
CHEMBL209821 NALUZOTAN IC50 = 3800.0 nM 5.42
CHEMBL207220 IC50 = 4000.0 nM 5.40
CHEMBL209324 IC50 > 5000.0 nM -
CHEMBL411941 CYCLORGDFV IC50 - -