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Assay Detail

CHEMBL740147

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 slices from the middle part of the mouse brain.
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Tissue Brain
Confidence 1 — Organism
Curated By Intermediate

Target

Mus musculus (CHEMBL375)
Type ORGANISM
Organism Mus musculus

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 9 5.88 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL287064 NOMELIDINE 2.0 1 7.00
CHEMBL367629 1 6.92
CHEMBL170027 1 6.30
CHEMBL172120 1 6.05
CHEMBL173745 NORZIMELIDINE 1 5.60
CHEMBL629 AMITRIPTYLINE 4.0 1 5.54
CHEMBL354646 1 5.21
CHEMBL445 NORTRIPTYLINE 4.0 1 5.17
CHEMBL174462 1 5.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL287064 NOMELIDINE IC50 = 100.0 nM 7.00
CHEMBL367629 IC50 = 120.0 nM 6.92
CHEMBL170027 IC50 = 500.0 nM 6.30
CHEMBL172120 IC50 = 900.0 nM 6.05
CHEMBL173745 NORZIMELIDINE IC50 = 2500.0 nM 5.60
CHEMBL629 AMITRIPTYLINE IC50 = 2900.0 nM 5.54
CHEMBL354646 IC50 = 6100.0 nM 5.21
CHEMBL445 NORTRIPTYLINE IC50 = 6700.0 nM 5.17
CHEMBL174462 IC50 = 7100.0 nM 5.15