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Assay Detail

CHEMBL4314363

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

Binding
Displacement of [3H]-imipramine from human serotonin transporter expressed in HEK293 cells membranes incubated for 30 mins by microbeta scintillation counting analysis
25
Total Activities
25
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

Synthesis and biological evaluation of new multi-target 3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives with potential antidepressant effect.
Wróbel MZ, Chodkowski A, Herold F, Marciniak M, Dawidowski M, Siwek A, Starowicz G, Stachowicz K, Szewczyk B, Nowak G, Belka M, Bączek T, Satała G, Bojarski AJ, Turło J.
Eur J Med Chem (2019) 183 : 111736 -111736
PubMed 31586817 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 7.03 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL439849 VILAZODONE 4.0 1 8.72
CHEMBL11 IMIPRAMINE 4.0 1 8.60
CHEMBL4571321 1 7.76
CHEMBL4553259 1 7.52
CHEMBL4515160 1 7.49
CHEMBL4571862 1 7.29
CHEMBL4456442 1 7.20
CHEMBL4591262 1 6.99
CHEMBL4451635 1 6.96
CHEMBL4567029 1 6.85
CHEMBL4470395 1 6.85
CHEMBL4470604 1 6.82
CHEMBL4587314 1 6.81
CHEMBL4454176 1 6.70
CHEMBL4461198 1 6.66
CHEMBL4591440 1 6.51
CHEMBL4472066 1 6.50
CHEMBL4482920 1 6.28
CHEMBL4483554 1 6.15
CHEMBL4572132 1 5.88
CHEMBL39 SEROTONIN 3.0 1 -
CHEMBL4474439 1 -
CHEMBL4461080 1 -
CHEMBL4567158 1 -
CHEMBL4437024 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL439849 VILAZODONE Ki = 1.9 nM 8.72
CHEMBL11 IMIPRAMINE Ki = 2.5 nM 8.60
CHEMBL4571321 Ki = 17.5 nM 7.76
CHEMBL4553259 Ki = 30.0 nM 7.52
CHEMBL4515160 Ki = 32.4 nM 7.49
CHEMBL4571862 Ki = 51.0 nM 7.29
CHEMBL4456442 Ki = 63.0 nM 7.20
CHEMBL4591262 Ki = 102.0 nM 6.99
CHEMBL4451635 Ki = 111.0 nM 6.96
CHEMBL4567029 Ki = 141.8 nM 6.85
CHEMBL4470395 Ki = 140.0 nM 6.85
CHEMBL4470604 Ki = 150.5 nM 6.82
CHEMBL4587314 Ki = 156.0 nM 6.81
CHEMBL4454176 Ki = 201.0 nM 6.70
CHEMBL4461198 Ki = 221.0 nM 6.66
CHEMBL4591440 Ki = 308.0 nM 6.51
CHEMBL4472066 Ki = 314.0 nM 6.50
CHEMBL4482920 Ki = 523.0 nM 6.28
CHEMBL4483554 Ki = 705.0 nM 6.15
CHEMBL4572132 Ki = 1313.0 nM 5.88
CHEMBL39 SEROTONIN Ki - -
CHEMBL4474439 Ki - -
CHEMBL4461080 Ki - -
CHEMBL4567158 Ki - -
CHEMBL4437024 Ki - -