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Assay Detail

CHEMBL3595874

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

Binding
Inhibition of human SERT expressed in CHOK1 cells incubated for 20 mins by [3H]-5-hydroxytryptamine uptake assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design, synthesis and biological evaluation of a novel series of peripheral-selective noradrenaline reuptake inhibitor.
Fujimori I, Yukawa T, Kamei T, Nakada Y, Sakauchi N, Yamada M, Ohba Y, Takiguchi M, Kuno M, Kamo I, Nakagawa H, Hamada T, Igari T, Okuda T, Yamamoto S, Tsukamoto T, Ishichi Y, Ueno H.
Bioorg Med Chem (2015) 23 : 5000 -5014
PubMed 26051602 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.80 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3593393 1 7.96
CHEMBL3593274 1 7.46
CHEMBL3593396 1 7.44
CHEMBL3593395 1 7.01
CHEMBL3593394 1 6.92
CHEMBL3593400 1 6.82
CHEMBL3593401 1 6.70
CHEMBL3593275 1 6.70
CHEMBL3593392 1 6.70
CHEMBL3593391 1 6.48
CHEMBL3593399 1 6.46
CHEMBL3593404 1 6.32
CHEMBL3593405 1 6.17
CHEMBL3593397 1 6.11
CHEMBL3593402 1 -
CHEMBL3593403 1 -
CHEMBL3593398 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3593393 IC50 = 11.0 nM 7.96
CHEMBL3593274 IC50 = 35.0 nM 7.46
CHEMBL3593396 IC50 = 36.0 nM 7.44
CHEMBL3593395 IC50 = 97.0 nM 7.01
CHEMBL3593394 IC50 = 120.0 nM 6.92
CHEMBL3593400 IC50 = 150.0 nM 6.82
CHEMBL3593401 IC50 = 200.0 nM 6.70
CHEMBL3593275 IC50 = 200.0 nM 6.70
CHEMBL3593392 IC50 = 200.0 nM 6.70
CHEMBL3593391 IC50 = 330.0 nM 6.48
CHEMBL3593399 IC50 = 350.0 nM 6.46
CHEMBL3593404 IC50 = 480.0 nM 6.32
CHEMBL3593405 IC50 = 680.0 nM 6.17
CHEMBL3593397 IC50 = 780.0 nM 6.11
CHEMBL3593402 IC50 > 1000.0 nM -
CHEMBL3593403 IC50 > 1000.0 nM -
CHEMBL3593398 IC50 > 1000.0 nM -