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Assay Detail

CHEMBL617483

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

Binding
Binding affinity against 5-hydroxytryptamine 2A receptor from rat forebrain using [3H]ketanserin as radioligand
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Exploring the relationship between binding modes of 9-(aminomethyl)-9,10-dihydroanthracene and cyproheptadine analogues at the 5-HT2A serotonin receptor.
Westkaemper RB, Runyon SP, Savage JE, Roth BL, Glennon RA.
Bioorg Med Chem Lett (2001) 11 : 563 -566
PubMed 11229772 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.84 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL516 CYPROHEPTADINE 4.0 1 8.80
CHEMBL152408 PIMETHIXENE 2.0 1 8.60
CHEMBL152407 1 8.40
CHEMBL152622 1 8.05
CHEMBL347536 1 7.89
CHEMBL348199 1 6.70
CHEMBL152289 1 6.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL516 CYPROHEPTADINE Ki = 1.6 nM 8.80
CHEMBL152408 PIMETHIXENE Ki = 2.5 nM 8.60
CHEMBL152407 Ki = 4.0 nM 8.40
CHEMBL152622 Ki = 9.0 nM 8.05
CHEMBL347536 Ki = 13.0 nM 7.89
CHEMBL348199 Ki = 199.0 nM 6.70
CHEMBL152289 Ki = 355.0 nM 6.45