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Assay Detail

CHEMBL3253107

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

Binding
Inhibition of 5-HT transporter in NMRI albino mouse brain assessed as [3H]5-HT accumulation in hypothalamus after 5 mins
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Tissue Hypothalamus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium-dependent serotonin transporter (CHEMBL4642)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Antidepressant agents. 9. 3,3-Diphenylcyclobutylamines, a new class of central stimulants.
Carnmalm B, Rämsby S, Renyi AL, Ross SB, Ogren SO.
J Med Chem (1978) 21 : 78 -82
PubMed 22757 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.61 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415 CLOMIPRAMINE 4.0 1 7.16
CHEMBL3251303 1 6.05
CHEMBL3251301 1 5.55
CHEMBL3251302 1 5.52
CHEMBL72 DESIPRAMINE 4.0 1 5.03
CHEMBL405 AMPHETAMINE 4.0 1 4.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415 CLOMIPRAMINE IC50 = 70.0 nM 7.16
CHEMBL3251303 IC50 = 900.0 nM 6.05
CHEMBL3251301 IC50 = 2800.0 nM 5.55
CHEMBL3251302 IC50 = 3000.0 nM 5.52
CHEMBL72 DESIPRAMINE IC50 = 9300.0 nM 5.03
CHEMBL405 AMPHETAMINE IC50 = 45000.0 nM 4.35