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Assay Detail

CHEMBL616895

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

Binding
Displacement of [3H]ketanserin from 5-hydroxytryptamine 2A receptor expressed NIH3T3 cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type NIH3T3
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Influence of chain length and N-alkylation on the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene.
Runyon SP, Savage JE, Taroua M, Roth BL, Glennon RA, Westkaemper RB.
Bioorg Med Chem Lett (2001) 11 : 655 -658
PubMed 11266163 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 6.85 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL516 CYPROHEPTADINE 4.0 1 8.80
CHEMBL348302 1 7.89
CHEMBL47482 1 7.70
CHEMBL346230 1 7.66
CHEMBL158780 1 7.50
CHEMBL73307 1 7.28
CHEMBL11 IMIPRAMINE 4.0 1 6.80
CHEMBL72 DESIPRAMINE 4.0 1 6.80
CHEMBL1317 DIDESMETHYLIMIPRAMINE 1 6.40
CHEMBL160893 1 6.32
CHEMBL160933 1 6.27
CHEMBL349543 1 6.14
CHEMBL158329 1 5.40
CHEMBL160610 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL516 CYPROHEPTADINE Ki = 1.6 nM 8.80
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
CHEMBL11 IMIPRAMINE Ki = 160.0 nM 6.80
CHEMBL72 DESIPRAMINE Ki = 160.0 nM 6.80
CHEMBL1317 DIDESMETHYLIMIPRAMINE Ki = 397.0 nM 6.40
CHEMBL160893 Ki = 480.0 nM 6.32
CHEMBL160933 Ki = 540.0 nM 6.27
CHEMBL349543 Ki = 721.0 nM 6.14
CHEMBL158329 Ki = 4000.0 nM 5.40
CHEMBL160610 Ki = 12000.0 nM 4.92