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

CHEMBL1073241

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

Binding
Displacement of [3H]ketanserin from human 5HT2A receptor expressed in cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis, structure-affinity relationships, and modeling of AMDA analogs at 5-HT2A and H1 receptors: structural factors contributing to selectivity.
Shah JR, Mosier PD, Roth BL, Kellogg GE, Westkaemper RB.
Bioorg Med Chem (2009) 17 : 6496 -6504
PubMed 19700330 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.53 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL348302 1 7.89
CHEMBL47482 1 7.70
CHEMBL346230 1 7.66
CHEMBL158780 1 7.50
CHEMBL73307 1 7.28
CHEMBL593988 1 7.08
CHEMBL595158 1 7.04
CHEMBL160893 1 6.32
CHEMBL160933 1 6.27
CHEMBL594138 1 6.12
CHEMBL608689 1 5.94
CHEMBL593494 1 5.82
CHEMBL610739 1 5.79
CHEMBL593734 1 5.59
CHEMBL10780 1 5.34
CHEMBL10602 1 5.13
CHEMBL609579 1 -
CHEMBL10961 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL348302 Ki = 13.0 nM 7.89
CHEMBL47482 Ki = 20.0 nM 7.70
CHEMBL346230 Ki = 22.0 nM 7.66
CHEMBL158780 Ki = 32.0 nM 7.50
CHEMBL73307 Ki = 52.0 nM 7.28
CHEMBL593988 Ki = 84.0 nM 7.08
CHEMBL595158 Ki = 92.0 nM 7.04
CHEMBL160893 Ki = 480.0 nM 6.32
CHEMBL160933 Ki = 540.0 nM 6.27
CHEMBL594138 Ki = 754.0 nM 6.12
CHEMBL608689 Ki = 1151.0 nM 5.94
CHEMBL593494 Ki = 1498.0 nM 5.82
CHEMBL610739 Ki = 1636.0 nM 5.79
CHEMBL593734 Ki = 2589.0 nM 5.59
CHEMBL10780 Ki = 4610.0 nM 5.34
CHEMBL10602 Ki = 7356.0 nM 5.13
CHEMBL609579 Ki > 10000.0 nM -
CHEMBL10961 Ki > 10000.0 nM -