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Assay Detail

CHEMBL781538

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

Functional
In vitro inhibition of the accumulation of (-)-[3H]-5-HT in synaptosomes from the rat brain cortex
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Brain
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Homoallylic amines related to zimeldine. A comparative study on neuronal serotonin and norepinephrine reuptake based on conformational analysis.
Högberg T, Ross SB, Ström P, Grunewald GL, Creese MW, Bunce JD.
J Med Chem (1988) 31 : 913 -919
PubMed 2966246 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.47 7.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL287064 NOMELIDINE 2.0 1 7.42
CHEMBL173745 NORZIMELIDINE 1 7.10
CHEMBL37744 ZIMELDINE 4.0 1 7.00
CHEMBL354646 1 6.66
CHEMBL170027 1 6.62
CHEMBL629 AMITRIPTYLINE 4.0 1 6.50
CHEMBL172120 1 6.30
CHEMBL367629 1 5.85
CHEMBL445 NORTRIPTYLINE 4.0 1 5.70
CHEMBL174462 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL287064 NOMELIDINE IC50 = 38.0 nM 7.42
CHEMBL173745 NORZIMELIDINE IC50 = 80.0 nM 7.10
CHEMBL37744 ZIMELDINE IC50 = 100.0 nM 7.00
CHEMBL354646 IC50 = 220.0 nM 6.66
CHEMBL170027 IC50 = 240.0 nM 6.62
CHEMBL629 AMITRIPTYLINE IC50 = 320.0 nM 6.50
CHEMBL172120 IC50 = 500.0 nM 6.30
CHEMBL367629 IC50 = 1400.0 nM 5.85
CHEMBL445 NORTRIPTYLINE IC50 = 2000.0 nM 5.70
CHEMBL174462 IC50 = 2600.0 nM 5.58