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Assay Detail

CHEMBL3756313

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

Binding
Displacement of [3H]citalopram from SERT in Sprague-Dawley rat whole brain membranes after 1 hr by liquid scintillation spectrometry
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium-dependent serotonin transporter (CHEMBL313)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

The influence of 5-HT(2A) activity on a 5-HT(2C) specific in vivo assay used for early identification of multiple acting SERT and 5-HT(2C) receptor ligands.
Éliás O, Nógrádi K, Domány G, Szakács Z, Kóti J, Szántay C, Tarcsay Á, Keserű GM, Gere A, Kiss B, Kurkó D, Kolok S, Némethy Z, Kapui Z, Hellinger É, Vastag M, Sághy K, Kedves R, Gyertyán I.
Bioorg Med Chem Lett (2016) 26 : 914 -920
PubMed 26748694 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.16 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3261686 1 8.05
CHEMBL3753894 1 7.69
CHEMBL3752844 1 7.58
CHEMBL3753681 1 7.53
CHEMBL3752059 1 7.43
CHEMBL3261690 1 7.42
CHEMBL3261695 1 7.39
CHEMBL3261693 1 7.21
CHEMBL3753516 1 7.18
CHEMBL3752465 1 7.18
CHEMBL3754137 1 7.03
CHEMBL3753283 1 6.96
CHEMBL3753329 1 6.68
CHEMBL3754784 1 6.29
CHEMBL14563 SB-242084 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3261686 Ki = 9.0 nM 8.05
CHEMBL3753894 Ki = 20.4 nM 7.69
CHEMBL3752844 Ki = 26.2 nM 7.58
CHEMBL3753681 Ki = 29.7 nM 7.53
CHEMBL3752059 Ki = 36.8 nM 7.43
CHEMBL3261690 Ki = 37.9 nM 7.42
CHEMBL3261695 Ki = 41.1 nM 7.39
CHEMBL3261693 Ki = 61.4 nM 7.21
CHEMBL3753516 Ki = 65.6 nM 7.18
CHEMBL3752465 Ki = 65.5 nM 7.18
CHEMBL3754137 Ki = 93.0 nM 7.03
CHEMBL3753283 Ki = 110.0 nM 6.96
CHEMBL3753329 Ki = 209.0 nM 6.68
CHEMBL3754784 Ki = 509.0 nM 6.29
CHEMBL14563 SB-242084 Ki = 1772.0 nM 5.75