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Assay Detail

CHEMBL1043671

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

Binding
Displacement of [3H]ketanserin from 5HT2A receptor in rat cerebral cortex after 20 mins by liquid scintillation counting
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

5-hydroxytryptamine receptor 2A (CHEMBL322)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and preliminary pharmacological evaluation of imidazo[2,1-f]purine-2,4-dione derivatives.
Zagórska A, Jurczyk S, Pawłowski M, Dybała M, Nowak G, Tatarczyńska E, Nikiforuk A, Chojnacka-Wójcik E.
Eur J Med Chem (2009) 44 : 4288 -4296
PubMed 19679379 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 6.47 7.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL566890 1 7.04
CHEMBL195047 1 6.53
CHEMBL567496 1 6.39
CHEMBL328292 1 6.31
CHEMBL566235 1 6.09
CHEMBL585105 1 -
CHEMBL565423 1 -
CHEMBL585300 1 -
CHEMBL585503 1 -
CHEMBL565405 1 -
CHEMBL584814 1 -
CHEMBL566022 1 -
CHEMBL566227 1 -
CHEMBL566891 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL566890 Ki = 91.5 nM 7.04
CHEMBL195047 Ki = 297.0 nM 6.53
CHEMBL567496 Ki = 403.0 nM 6.39
CHEMBL328292 Ki = 486.0 nM 6.31
CHEMBL566235 Ki = 813.5 nM 6.09
CHEMBL585105 Ki > 1000.0 nM -
CHEMBL565423 Ki > 1000.0 nM -
CHEMBL585300 Ki > 1000.0 nM -
CHEMBL585503 Ki > 1000.0 nM -
CHEMBL565405 Ki > 1000.0 nM -
CHEMBL584814 Ki > 1000.0 nM -
CHEMBL566022 Ki - -
CHEMBL566227 Ki - -
CHEMBL566891 Ki - -