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Assay Detail

CHEMBL893718

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

Binding
Displacement of [3H]citalopram from human SERT expressed in HEK293 cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Conformationally restricted homotryptamines 3. Indole tetrahydropyridines and cyclohexenylamines as selective serotonin reuptake inhibitors.
Deskus JA, Epperson JR, Sloan CP, Cipollina JA, Dextraze P, Qian-Cutrone J, Gao Q, Ma B, Beno BR, Mattson GK, Molski TF, Krause RG, Taber MT, Lodge NJ, Mattson RJ.
Bioorg Med Chem Lett (2007) 17 : 3099 -3104
PubMed 17391962 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.49 9.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL234706 1 9.14
CHEMBL396537 1 9.00
CHEMBL234705 1 8.96
CHEMBL390432 1 8.80
CHEMBL231809 1 8.51
CHEMBL396540 1 8.28
CHEMBL234927 1 7.85
CHEMBL234928 1 7.72
CHEMBL283899 1 7.72
CHEMBL283416 1 7.40
CHEMBL394356 1 6.82
CHEMBL27025 1 6.80
CHEMBL27227 1 6.68
CHEMBL283185 1 6.62
CHEMBL26655 1 6.16
CHEMBL285777 1 6.14
CHEMBL234291 1 6.11
CHEMBL442534 1 6.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL234706 IC50 = 0.72 nM 9.14
CHEMBL396537 IC50 = 1.0 nM 9.00
CHEMBL234705 IC50 = 1.1 nM 8.96
CHEMBL390432 IC50 = 1.6 nM 8.80
CHEMBL231809 IC50 = 3.1 nM 8.51
CHEMBL396540 IC50 = 5.3 nM 8.28
CHEMBL234927 IC50 = 14.0 nM 7.85
CHEMBL234928 IC50 = 19.0 nM 7.72
CHEMBL283899 IC50 = 19.0 nM 7.72
CHEMBL283416 IC50 = 40.0 nM 7.40
CHEMBL394356 IC50 = 150.0 nM 6.82
CHEMBL27025 IC50 = 160.0 nM 6.80
CHEMBL27227 IC50 = 210.0 nM 6.68
CHEMBL283185 IC50 = 240.0 nM 6.62
CHEMBL26655 IC50 = 690.0 nM 6.16
CHEMBL285777 IC50 = 730.0 nM 6.14
CHEMBL234291 IC50 = 770.0 nM 6.11
CHEMBL442534 IC50 = 910.0 nM 6.04