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Assay Detail

CHEMBL978153

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

Binding
Inhibition of [3H]5HT reuptake at human serotonin transporter expressed in HEK293 cells by scintillation counting
23
Total Activities
23
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

N-Benzyl-N-(pyrrolidin-3-yl)carboxamides as a new class of selective dual serotonin/noradrenaline reuptake inhibitors.
Wakenhut F, Fish PV, Fray MJ, Gurrell I, Mills JE, Stobie A, Whitlock GA.
Bioorg Med Chem Lett (2008) 18 : 4308 -4311
PubMed 18625557 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.49 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL477374 1 8.30
CHEMBL450813 1 8.30
CHEMBL247733 1 8.05
CHEMBL476954 1 7.92
CHEMBL513139 1 7.89
CHEMBL448900 1 7.77
CHEMBL477584 1 7.62
CHEMBL512967 1 7.60
CHEMBL446281 1 7.58
CHEMBL469068 1 7.57
CHEMBL513313 1 7.48
CHEMBL512472 1 7.42
CHEMBL513360 1 7.39
CHEMBL449145 1 7.39
CHEMBL477580 1 7.36
CHEMBL466963 1 7.14
CHEMBL517963 1 7.04
CHEMBL469222 1 7.03
CHEMBL513884 1 6.91
CHEMBL518580 1 6.79
CHEMBL469233 1 6.71
CHEMBL477586 1 -
CHEMBL476116 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL477374 IC50 = 5.0 nM 8.30
CHEMBL450813 IC50 = 5.0 nM 8.30
CHEMBL247733 IC50 = 9.0 nM 8.05
CHEMBL476954 IC50 = 12.0 nM 7.92
CHEMBL513139 IC50 = 13.0 nM 7.89
CHEMBL448900 IC50 = 17.0 nM 7.77
CHEMBL477584 IC50 = 24.0 nM 7.62
CHEMBL512967 IC50 = 25.0 nM 7.60
CHEMBL446281 IC50 = 26.0 nM 7.58
CHEMBL469068 IC50 = 27.0 nM 7.57
CHEMBL513313 IC50 = 33.0 nM 7.48
CHEMBL512472 IC50 = 38.0 nM 7.42
CHEMBL513360 IC50 = 41.0 nM 7.39
CHEMBL449145 IC50 = 41.0 nM 7.39
CHEMBL477580 IC50 = 44.0 nM 7.36
CHEMBL466963 IC50 = 72.0 nM 7.14
CHEMBL517963 IC50 = 91.0 nM 7.04
CHEMBL469222 IC50 = 93.0 nM 7.03
CHEMBL513884 IC50 = 123.0 nM 6.91
CHEMBL518580 IC50 = 161.0 nM 6.79
CHEMBL469233 IC50 = 195.0 nM 6.71
CHEMBL477586 IC50 > 400.0 nM -
CHEMBL476116 IC50 > 400.0 nM -