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Assay Detail

CHEMBL1060392

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

Functional
Antagonist activity at human 5HT transporter expressed in staurosporine treated human JAR cells
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type JAR
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Sodium-dependent serotonin transporter (CHEMBL228)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, potency, and in vivo evaluation of 2-piperazin-1-ylquinoline analogues as dual serotonin reuptake inhibitors and serotonin 5-HT1A receptor antagonists.
Zhou D, Stack GP, Lo J, Failli AA, Evrard DA, Harrison BL, Hatzenbuhler NT, Tran M, Croce S, Yi S, Golembieski J, Hornby GA, Lai M, Lin Q, Schechter LE, Smith DL, Shilling AD, Huselton C, Mitchell P, Beyer CE, Andree TH.
J Med Chem (2009) 52 : 4955 -4959
PubMed 19719241 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.84 6.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL562248 1 6.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL562248 IC50 = 145.0 nM 6.84