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Assay Detail

CHEMBL4815626

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

Binding
Displacement of [3H]-citalopram from human SERT receptor incubated for 1 hr by liquid scintillation counting method
14
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

New dual 5-HT1A and 5-HT7 receptor ligands derived from SYA16263.
Ofori E, Onyameh EK, Gonela UM, Voshavar C, Bricker B, Swanson TL, Eshleman AJ, Schmachtenberg JL, Bloom SH, Janowsky AJ, Ablordeppey SY.
Eur J Med Chem (2021) 214 : 113243 -113243
PubMed 33582388 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 6.00 6.61

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4859722 2 6.61
CHEMBL4866053 1 6.41
CHEMBL1112 ARIPIPRAZOLE 4.0 1 5.97
CHEMBL4857597 2 5.96
CHEMBL4857665 2 5.72
CHEMBL4865591 2 5.58
CHEMBL4846823 2 -
CHEMBL4871868 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4859722 Ki = 248.0 nM 6.61
CHEMBL4859722 Ki = 245.47 nM 6.61
CHEMBL4866053 Ki = 392.0 nM 6.41
CHEMBL1112 ARIPIPRAZOLE Ki = 1080.0 nM 5.97
CHEMBL4857597 Ki = 1096.48 nM 5.96
CHEMBL4857597 Ki = 1143.0 nM 5.94
CHEMBL4857665 Ki = 1905.46 nM 5.72
CHEMBL4857665 Ki = 2184.0 nM 5.66
CHEMBL4865591 Ki = 2630.27 nM 5.58
CHEMBL4865591 Ki = 3064.6 nM 5.51
CHEMBL4846823 Ki > 10000.0 nM -
CHEMBL4871868 Ki > 10000.0 nM -
CHEMBL4846823 Ki > 10000.0 nM -
CHEMBL4871868 Ki > 10000.0 nM -