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Assay Detail

CHEMBL1259259

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

Binding
Displacement of [3H]Ketanserin from 5-HT2 receptor in pig cortex membranes
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2A (CHEMBL2490)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Novel pyridylmethylamines as highly selective 5-HT(1A) superagonists.
Bollinger S, Hübner H, Heinemann FW, Meyer K, Gmeiner P.
J Med Chem (2010) 53 : 7167 -7179
PubMed 20860381 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 4.58 4.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1259071 1 4.75
CHEMBL1259241 1 4.66
CHEMBL45305 BEFIRADOL 2.0 1 4.64
CHEMBL1258999 1 4.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1259071 Ki = 18000.0 nM 4.75
CHEMBL1259241 Ki = 22000.0 nM 4.66
CHEMBL45305 BEFIRADOL Ki = 23000.0 nM 4.64
CHEMBL1258999 Ki = 53000.0 nM 4.28