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Assay Detail

CHEMBL619952

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

Binding
Binding affinity to human cloned 5-HT6 receptor in HeLa cells using [3H]- LSD as radioligand
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides with high affinity and selectivity for the 5-HT(6) receptor.
Bromidge SM, Griffith K, Heightman TD, Jennings A, King FD, Moss SF, Newman H, Riley G, Routledge C, Serafinowska HT, Thomas DR.
Bioorg Med Chem Lett (2001) 11 : 2843 -2846
PubMed 11597412 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 8.96 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL97637 1 9.30
CHEMBL316081 1 9.00
CHEMBL97596 1 9.00
CHEMBL318018 1 9.00
CHEMBL97211 1 8.90
CHEMBL98965 1 8.90
CHEMBL95823 1 8.90
CHEMBL97158 1 8.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL97637 Ki = 0.5012 nM 9.30
CHEMBL316081 Ki = 1.0 nM 9.00
CHEMBL97596 Ki = 1.0 nM 9.00
CHEMBL318018 Ki = 1.0 nM 9.00
CHEMBL97211 Ki = 1.259 nM 8.90
CHEMBL98965 Ki = 1.259 nM 8.90
CHEMBL95823 Ki = 1.259 nM 8.90
CHEMBL97158 Ki = 1.995 nM 8.70