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Assay Detail

CHEMBL834018

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

Functional
Inhibitory concentration against serotonin transporter protein (SERT) expressed in HEK293 cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Homotryptamines as potent and selective serotonin reuptake inhibitors (SSRIs).
Schmitz WD, Denhart DJ, Brenner AB, Ditta JL, Mattson RJ, Mattson GK, Molski TF, Macor JE.
Bioorg Med Chem Lett (2005) 15 : 1619 -1621
PubMed 15745809 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.47 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL179767 1 8.70
CHEMBL180630 1 8.70
CHEMBL361949 1 8.40
CHEMBL362170 1 8.15
CHEMBL183238 1 7.96
CHEMBL183488 1 7.77
CHEMBL2113005 1 7.75
CHEMBL182386 1 7.54
CHEMBL183542 1 7.51
CHEMBL180537 1 7.50
CHEMBL361622 1 7.44
CHEMBL360575 1 7.24
CHEMBL368229 1 5.96
CHEMBL416526 BUFOTENINE 1 5.92
CHEMBL2113003 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL179767 IC50 = 2.0 nM 8.70
CHEMBL180630 IC50 = 2.0 nM 8.70
CHEMBL361949 IC50 = 4.0 nM 8.40
CHEMBL362170 IC50 = 7.0 nM 8.15
CHEMBL183238 IC50 = 11.0 nM 7.96
CHEMBL183488 IC50 = 17.0 nM 7.77
CHEMBL2113005 IC50 = 18.0 nM 7.75
CHEMBL182386 IC50 = 29.0 nM 7.54
CHEMBL183542 IC50 = 31.0 nM 7.51
CHEMBL180537 IC50 = 32.0 nM 7.50
CHEMBL361622 IC50 = 36.0 nM 7.44
CHEMBL360575 IC50 = 58.0 nM 7.24
CHEMBL368229 IC50 = 1100.0 nM 5.96
CHEMBL416526 BUFOTENINE IC50 = 1200.0 nM 5.92
CHEMBL2113003 IC50 = 3200.0 nM 5.50