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Assay Detail

CHEMBL617253

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

Binding
Binding affinity to human cloned 5-hydroxytryptamine 2A receptor in HEK 293 cells using [3H]- ketanserin as radioligand
9
Total Activities
9
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 2A (CHEMBL224)
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 9 6.10 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL97637 1 6.30
CHEMBL316081 1 6.00
CHEMBL97596 1 6.00
CHEMBL261917 1 -
CHEMBL97211 1 -
CHEMBL97158 1 -
CHEMBL318018 1 -
CHEMBL98965 1 -
CHEMBL95823 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL97637 Ki = 501.19 nM 6.30
CHEMBL316081 Ki = 1000.0 nM 6.00
CHEMBL97596 Ki = 1000.0 nM 6.00
CHEMBL261917 Ki < 3162.28 nM -
CHEMBL97211 Ki < 1995.26 nM -
CHEMBL97158 Ki < 2511.89 nM -
CHEMBL318018 Ki < 1995.26 nM -
CHEMBL98965 Ki < 1258.93 nM -
CHEMBL95823 Ki < 2511.89 nM -