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Assay Detail

CHEMBL2382973

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 cell membranes
15
Total Activities
15
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 Autocuration

Target

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

Publication

Conformationally restricted homotryptamines. Part 6: indole-5-cycloalkyl methylamines as selective serotonin reuptake inhibitors.
Ditta JL, Denhart DJ, Deskus JA, Epperson JR, Meng Z, Gao Q, Mattson GK, Lapaglia MA, Taber MT, Molski TF, Lodge NJ, Mattson RJ, Macor JE.
Bioorg Med Chem Lett (2013) 23 : 2948 -2950
PubMed 23578689 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.44 9.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL196468 1 9.25
CHEMBL539470 1 8.96
CHEMBL2380980 1 8.42
CHEMBL2380975 1 8.37
CHEMBL2380983 1 8.22
CHEMBL2380971 1 7.75
CHEMBL2380972 1 7.19
CHEMBL2380979 1 7.01
CHEMBL2380974 1 6.85
CHEMBL2380976 1 6.70
CHEMBL2380978 1 6.58
CHEMBL2380973 1 6.52
CHEMBL2380981 1 6.24
CHEMBL2380977 1 6.15
CHEMBL2380982 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL196468 IC50 = 0.56 nM 9.25
CHEMBL539470 IC50 = 1.1 nM 8.96
CHEMBL2380980 IC50 = 3.8 nM 8.42
CHEMBL2380975 IC50 = 4.3 nM 8.37
CHEMBL2380983 IC50 = 6.0 nM 8.22
CHEMBL2380971 IC50 = 18.0 nM 7.75
CHEMBL2380972 IC50 = 64.0 nM 7.19
CHEMBL2380979 IC50 = 97.0 nM 7.01
CHEMBL2380974 IC50 = 140.0 nM 6.85
CHEMBL2380976 IC50 = 200.0 nM 6.70
CHEMBL2380978 IC50 = 260.0 nM 6.58
CHEMBL2380973 IC50 = 300.0 nM 6.52
CHEMBL2380981 IC50 = 570.0 nM 6.24
CHEMBL2380977 IC50 = 710.0 nM 6.15
CHEMBL2380982 IC50 > 1000.0 nM -