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Assay Detail

CHEMBL5136476

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

Binding
Inhibition of human SERT transfected in HEK cells using APP+ as fluorescent substrate preincubated for 1 hr followed by substrate addition and measured after 30 mins by fluorescence plate reader assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Ibogaine and Their Analogs as Therapeutics for Neurological and Psychiatric Disorders.
Kargbo RB.
ACS Med Chem Lett (2022) 13 : 888 -890
PubMed 35707155 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.53 8.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5188930 1 8.29
CHEMBL5175119 1 7.58
CHEMBL5207764 1 7.23
CHEMBL5201219 1 7.10
CHEMBL5202868 1 6.55
CHEMBL5184088 1 6.48
CHEMBL1215855 1 6.30
CHEMBL5188726 1 6.17
CHEMBL5180373 1 6.04
CHEMBL5171433 1 5.82
CHEMBL5176306 1 5.72
CHEMBL5207655 1 5.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5188930 IC50 = 5.1 nM 8.29
CHEMBL5175119 IC50 = 26.0 nM 7.58
CHEMBL5207764 IC50 = 59.0 nM 7.23
CHEMBL5201219 IC50 = 80.0 nM 7.10
CHEMBL5202868 IC50 = 280.0 nM 6.55
CHEMBL5184088 IC50 = 330.0 nM 6.48
CHEMBL1215855 IC50 = 500.0 nM 6.30
CHEMBL5188726 IC50 = 670.0 nM 6.17
CHEMBL5180373 IC50 = 910.0 nM 6.04
CHEMBL5171433 IC50 = 1500.0 nM 5.82
CHEMBL5176306 IC50 = 1900.0 nM 5.72
CHEMBL5207655 IC50 = 9000.0 nM 5.05