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Assay Detail

CHEMBL880240

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

Binding
Displacement of [3H]LSD binding to cloned human 5-hydroxytryptamine 6 receptor expressed in HEK cells
15
Total Activities
15
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 Expert

Target

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

Publication

2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists.
Mattsson C, Sonesson C, Sandahl A, Greiner HE, Gassen M, Plaschke J, Leibrock J, Böttcher H.
Bioorg Med Chem Lett (2005) 15 : 3230 -4234
PubMed 16055331 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.41 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL414668 1 8.70
CHEMBL364005 1 8.13
CHEMBL193351 1 8.00
CHEMBL194843 1 7.52
CHEMBL195759 1 7.52
CHEMBL363417 1 7.40
CHEMBL365751 1 7.40
CHEMBL435126 1 7.40
CHEMBL364271 1 7.30
CHEMBL371203 1 7.22
CHEMBL370436 1 7.16
CHEMBL194305 1 7.10
CHEMBL18785 RU-24969 1 7.10
CHEMBL195239 1 7.00
CHEMBL194908 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL414668 IC50 = 2.0 nM 8.70
CHEMBL364005 IC50 = 7.4 nM 8.13
CHEMBL193351 IC50 = 10.0 nM 8.00
CHEMBL194843 IC50 = 30.0 nM 7.52
CHEMBL195759 IC50 = 30.0 nM 7.52
CHEMBL363417 IC50 = 40.0 nM 7.40
CHEMBL365751 IC50 = 40.0 nM 7.40
CHEMBL435126 IC50 = 40.0 nM 7.40
CHEMBL364271 IC50 = 50.0 nM 7.30
CHEMBL371203 IC50 = 60.0 nM 7.22
CHEMBL370436 IC50 = 70.0 nM 7.16
CHEMBL194305 IC50 = 80.0 nM 7.10
CHEMBL18785 RU-24969 IC50 = 79.0 nM 7.10
CHEMBL195239 IC50 = 100.0 nM 7.00
CHEMBL194908 IC50 = 600.0 nM 6.22