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Assay Detail

CHEMBL1039634

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

Binding
Displacement of [3H]ketanserin from 5HT2A receptor in rat cortex
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characterization.
Butini S, Budriesi R, Hamon M, Morelli E, Gemma S, Brindisi M, Borrelli G, Novellino E, Fiorini I, Ioan P, Chiarini A, Cagnotto A, Mennini T, Fracasso C, Caccia S, Campiani G.
J Med Chem (2009) 52 : 6946 -6950
PubMed 19831400 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 5.67 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18772 QUIPAZINE 2.0 1 6.10
CHEMBL39 SEROTONIN 3.0 1 5.90
CHEMBL582992 1 5.01
CHEMBL566522 1 -
CHEMBL571046 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18772 QUIPAZINE Ki = 794.0 nM 6.10
CHEMBL39 SEROTONIN Ki = 1258.0 nM 5.90
CHEMBL582992 Ki = 9806.0 nM 5.01
CHEMBL566522 Ki > 10000.0 nM -
CHEMBL571046 Ki > 10000.0 nM -