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Assay Detail

CHEMBL2379472

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

Binding
Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK cell membranes after 1 hr by liquid scintillation counting analysis
14
Total Activities
14
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

5-hydroxytryptamine receptor 6 (CHEMBL3371)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationship of 5-chloro-2-methyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole analogues as 5-HT(6) receptor agonists.
Mattsson C, Svensson P, Boettcher H, Sonesson C.
Eur J Med Chem (2013) 63 : 578 -588
PubMed 23542166 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.26 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2376488 1 8.05
CHEMBL2376487 1 8.00
CHEMBL2376482 1 8.00
CHEMBL26379 1 7.70
CHEMBL2376486 1 7.70
CHEMBL2376483 1 7.52
CHEMBL2376492 1 7.40
CHEMBL2376484 1 7.30
CHEMBL2376560 1 7.10
CHEMBL2376493 1 7.00
CHEMBL2376489 1 7.00
CHEMBL1550957 1 6.70
CHEMBL2376490 1 6.16
CHEMBL2376491 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2376488 IC50 = 9.0 nM 8.05
CHEMBL2376487 IC50 = 10.0 nM 8.00
CHEMBL2376482 IC50 = 10.0 nM 8.00
CHEMBL26379 IC50 = 20.0 nM 7.70
CHEMBL2376486 IC50 = 20.0 nM 7.70
CHEMBL2376483 IC50 = 30.0 nM 7.52
CHEMBL2376492 IC50 = 40.0 nM 7.40
CHEMBL2376484 IC50 = 50.0 nM 7.30
CHEMBL2376560 IC50 = 80.0 nM 7.10
CHEMBL2376493 IC50 = 100.0 nM 7.00
CHEMBL2376489 IC50 = 100.0 nM 7.00
CHEMBL1550957 IC50 = 200.0 nM 6.70
CHEMBL2376490 IC50 = 700.0 nM 6.16
CHEMBL2376491 IC50 = 1000.0 nM 6.00