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Assay Detail

CHEMBL3756315

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

Binding
Displacement of [3H]ketanserin from 5HT2A in Wistar rat frontal cortex membranes after 1 hr by liquid scintillation spectrometry
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Frontal cortex
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

The influence of 5-HT(2A) activity on a 5-HT(2C) specific in vivo assay used for early identification of multiple acting SERT and 5-HT(2C) receptor ligands.
Éliás O, Nógrádi K, Domány G, Szakács Z, Kóti J, Szántay C, Tarcsay Á, Keserű GM, Gere A, Kiss B, Kurkó D, Kolok S, Némethy Z, Kapui Z, Hellinger É, Vastag M, Sághy K, Kedves R, Gyertyán I.
Bioorg Med Chem Lett (2016) 26 : 914 -920
PubMed 26748694 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.20 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3753894 1 8.52
CHEMBL3753681 1 8.00
CHEMBL3752844 1 7.23
CHEMBL3752465 1 6.86
CHEMBL3261695 1 6.63
CHEMBL3261686 1 6.62
CHEMBL14563 SB-242084 1 6.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3753894 Ki = 3.0 nM 8.52
CHEMBL3753681 Ki = 9.9 nM 8.00
CHEMBL3752844 Ki = 58.4 nM 7.23
CHEMBL3752465 Ki = 138.0 nM 6.86
CHEMBL3261695 Ki = 233.0 nM 6.63
CHEMBL3261686 Ki = 239.0 nM 6.62
CHEMBL14563 SB-242084 Ki = 274.0 nM 6.56