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Assay Detail

CHEMBL616875

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

Binding
Binding affinity towards 5-hydroxytryptamine 2A receptor (human cloned receptor) in HEK 293 cells using [3H]ketanserin as radioligand.
10
Total Activities
10
Compounds Tested
2
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

A novel, potent, and selective 5-HT(7) antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl) phen ol (SB-269970).
Lovell PJ, Bromidge SM, Dabbs S, Duckworth DM, Forbes IT, Jennings AJ, King FD, Middlemiss DN, Rahman SK, Saunders DV, Collin LL, Hagan JJ, Riley GJ, Thomas DR.
J Med Chem (2000) 43 : 342 -345
PubMed 10669560 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 5.80 5.80
Log Ki 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL94984 1 5.80
CHEMBL332701 1 -
CHEMBL94261 1 -
CHEMBL282199 1 -
CHEMBL114012 1 -
CHEMBL152595 1 -
CHEMBL12624 SB-258741 1 -
CHEMBL1788231 1 -
CHEMBL333784 1 -
CHEMBL116448 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL94984 Ki = 1584.89 nM 5.80
CHEMBL332701 Log Ki - -
CHEMBL94261 Log Ki - -
CHEMBL282199 Ki < 10000.0 nM -
CHEMBL114012 Ki < 3162.28 nM -
CHEMBL152595 Log Ki - -
CHEMBL12624 SB-258741 Ki < 5011.87 nM -
CHEMBL1788231 Ki < 2511.89 nM -
CHEMBL333784 Ki < 1000.0 nM -
CHEMBL116448 Ki < 5011.87 nM -