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Assay Detail

CHEMBL882908

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

Binding
Inhibitory concentration against serotonin transporter
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Sodium-dependent serotonin transporter (CHEMBL228)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Designed multiple ligands. An emerging drug discovery paradigm.
Morphy R, Rankovic Z.
J Med Chem (2005) 48 : 6523 -6543
PubMed 16220969 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.74 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL83617 1 9.96
CHEMBL197982 1 8.68
CHEMBL197696 1 8.22
CHEMBL326466 1 8.05
CHEMBL268258 1 7.89
CHEMBL9831 1 7.68
CHEMBL194372 1 7.38
CHEMBL259209 MILNACIPRAN 4.0 1 7.00
CHEMBL198072 1 6.92
CHEMBL198045 1 6.80
CHEMBL365183 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL83617 IC50 = 0.11 nM 9.96
CHEMBL197982 IC50 = 2.1 nM 8.68
CHEMBL197696 IC50 = 6.0 nM 8.22
CHEMBL326466 IC50 = 9.0 nM 8.05
CHEMBL268258 IC50 = 13.0 nM 7.89
CHEMBL9831 IC50 = 21.0 nM 7.68
CHEMBL194372 IC50 = 42.0 nM 7.38
CHEMBL259209 MILNACIPRAN IC50 = 100.0 nM 7.00
CHEMBL198072 IC50 = 120.0 nM 6.92
CHEMBL198045 IC50 = 160.0 nM 6.80
CHEMBL365183 IC50 = 270.0 nM 6.57