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Assay Detail

CHEMBL809444

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

Binding
Inhibition of 0.2 nM [3H]paroxetine binding to Serotonin transporter
13
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Sodium-dependent serotonin transporter (CHEMBL313)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

3alpha-(4-Substituted phenyl)nortropane-2beta-carboxylic acid methyl esters show selective binding at the norepinephrine transporter.
Blough BE, Holmquist CR, Abraham P, Kuhar MJ, Carroll FI.
Bioorg Med Chem Lett (2000) 10 : 2445 -2447
PubMed 11078197 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.64 9.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL81525 2 9.42
CHEMBL306208 2 8.40
CHEMBL80515 2 8.21
CHEMBL80262 2 7.92
CHEMBL82027 2 7.66
CHEMBL2079586 2 7.16
CHEMBL370805 COCAINE 4.0 1 7.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL81525 Ki = 0.38 nM 9.42
CHEMBL306208 Ki = 4.0 nM 8.40
CHEMBL81525 Ki = 4.8 nM 8.32
CHEMBL80515 Ki = 6.24 nM 8.21
CHEMBL80515 Ki = 8.4 nM 8.08
CHEMBL80262 Ki = 12.0 nM 7.92
CHEMBL82027 Ki = 22.0 nM 7.66
CHEMBL80262 Ki = 46.0 nM 7.34
CHEMBL2079586 Ki = 69.0 nM 7.16
CHEMBL306208 Ki = 91.0 nM 7.04
CHEMBL370805 COCAINE Ki = 95.0 nM 7.02
CHEMBL82027 Ki = 390.0 nM 6.41
CHEMBL2079586 Ki = 460.0 nM 6.34