Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL994217

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

Binding
Displacement of [3H]ketanserein from 5HT2A receptor F340L mutant expressed in NIH3T3 cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type NIH3T3
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potential modes of interaction of 9-aminomethyl-9,10-dihydroanthracene (AMDA) derivatives with the 5-HT2A receptor: a ligand structure-affinity relationship, receptor mutagenesis and receptor modeling investigation.
Runyon SP, Mosier PD, Roth BL, Glennon RA, Westkaemper RB.
J Med Chem (2008) 51 : 6808 -6828
PubMed 18847250 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.39 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL51 KETANSERIN 3.0 1 9.64
CHEMBL85882 1 8.74
CHEMBL444761 1 8.46
CHEMBL47482 1 7.24
CHEMBL10780 1 5.38
CHEMBL6616 1 4.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL51 KETANSERIN Ki = 0.23 nM 9.64
CHEMBL85882 Ki = 1.8 nM 8.74
CHEMBL444761 Ki = 3.5 nM 8.46
CHEMBL47482 Ki = 57.0 nM 7.24
CHEMBL10780 Ki = 4140.0 nM 5.38
CHEMBL6616 Ki = 13700.0 nM 4.86