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Assay Detail

CHEMBL5318152

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

Binding
Inhibition of SERT receptor (unknown origin)
9
Total Activities
9
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

Deciphering Nonbioavailable Substructures Improves the Bioavailability of Antidepressants by Serotonin Transporter.
Wang ZZ, Yi C, Huang JJ, Xu TF, Chen KZ, Wang ZS, Xue YP, Lu JL, Nie B, Zhang YJ, Jin CF, Hao GF.
J Med Chem (2023) 66 : 371 -383
PubMed 36598095 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 9.16 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5420565 1 9.49
CHEMBL5431204 1 9.46
CHEMBL439849 VILAZODONE 4.0 1 9.32
CHEMBL5438420 1 9.24
CHEMBL2104993 VORTIOXETINE 4.0 1 8.27
CHEMBL5413412 1 -
CHEMBL5394701 1 -
CHEMBL5423624 1 -
CHEMBL5407190 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5420565 IC50 = 0.32 nM 9.49
CHEMBL5431204 IC50 = 0.35 nM 9.46
CHEMBL439849 VILAZODONE IC50 = 0.48 nM 9.32
CHEMBL5438420 IC50 = 0.58 nM 9.24
CHEMBL2104993 VORTIOXETINE IC50 = 5.4 nM 8.27
CHEMBL5413412 IC50 < 2.0 nM -
CHEMBL5394701 IC50 < 2.0 nM -
CHEMBL5423624 IC50 < 2.0 nM -
CHEMBL5407190 IC50 < 2.0 nM -