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Assay Detail

CHEMBL792305

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

Binding
Inhibition of [3H]- NE reuptake into rat hippocampal synaptosomes
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Hippocampus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Norepinephrine transporter (CHEMBL304)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis of a potent wide-spectrum serotonin-, norepinephrine-, dopamine-reuptake inhibitor (SNDRI) and a species-selective dopamine-reuptake inhibitor based on the gamma-amino alcohol functional group.
Carlier PR, Lo MM, Lo PC, Richelson E, Tatsumi M, Reynolds IJ, Sharma TA.
Bioorg Med Chem Lett (1998) 8 : 487 -492
PubMed 9871604 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.70 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL641 ATOMOXETINE 4.0 1 9.15
CHEMBL539564 1 8.11
CHEMBL543925 1 8.00
CHEMBL539050 1 7.82
CHEMBL490 PAROXETINE 4.0 1 7.48
CHEMBL545557 1 7.36
CHEMBL637 VENLAFAXINE 4.0 1 6.86
CHEMBL41 FLUOXETINE 4.0 1 6.84
CHEMBL306700 VILOXAZINE 4.0 1 6.77
CHEMBL809 SERTRALINE 4.0 1 6.66
CHEMBL538053 1 6.66
CHEMBL540333 1 6.48
CHEMBL623 NEFAZODONE 4.0 1 6.24
CHEMBL542501 1 6.08
CHEMBL556025 1 6.00
CHEMBL555280 1 5.42
CHEMBL542746 1 5.24
CHEMBL539054 1 5.07
CHEMBL544633 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL641 ATOMOXETINE Ki = 0.7 nM 9.15
CHEMBL539564 Ki = 7.7 nM 8.11
CHEMBL543925 Ki = 10.0 nM 8.00
CHEMBL539050 Ki = 15.0 nM 7.82
CHEMBL490 PAROXETINE Ki = 33.0 nM 7.48
CHEMBL545557 Ki = 44.0 nM 7.36
CHEMBL637 VENLAFAXINE Ki = 138.0 nM 6.86
CHEMBL41 FLUOXETINE Ki = 143.0 nM 6.84
CHEMBL306700 VILOXAZINE Ki = 170.0 nM 6.77
CHEMBL809 SERTRALINE Ki = 220.0 nM 6.66
CHEMBL538053 Ki = 220.0 nM 6.66
CHEMBL540333 Ki = 330.0 nM 6.48
CHEMBL623 NEFAZODONE Ki = 570.0 nM 6.24
CHEMBL542501 Ki = 830.0 nM 6.08
CHEMBL556025 Ki = 990.0 nM 6.00
CHEMBL555280 Ki = 3800.0 nM 5.42
CHEMBL542746 Ki = 5780.0 nM 5.24
CHEMBL539054 Ki = 8600.0 nM 5.07
CHEMBL544633 Ki = 8500.0 nM 5.07