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Assay Detail

CHEMBL617345

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Binding
Binding affinity towards 5-hydroxytryptamine 2A receptor using [3H]ketanserin
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structural determinants for high 5-HT(2A) receptor affinity of spiro[9,10-dihydroanthracene]-9,3(')-pyrrolidine (SpAMDA).
Peddi S, Roth BL, Glennon RA, Westkaemper RB.
Bioorg Med Chem Lett (2004) 14 : 2279 -2283
PubMed 15081025 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.27 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL516 CYPROHEPTADINE 4.0 1 8.52
CHEMBL307956 1 8.40
CHEMBL47482 1 7.70
CHEMBL73307 1 7.28
CHEMBL46566 1 7.19
CHEMBL11 IMIPRAMINE 4.0 1 7.03
CHEMBL74766 1 7.00
CHEMBL72611 1 6.96
CHEMBL76281 1 5.34
CHEMBL73783 1 -
CHEMBL75207 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL516 CYPROHEPTADINE Ki = 3.0 nM 8.52
CHEMBL307956 Ki = 4.0 nM 8.40
CHEMBL47482 Ki = 20.0 nM 7.70
CHEMBL73307 Ki = 52.0 nM 7.28
CHEMBL46566 Ki = 65.0 nM 7.19
CHEMBL11 IMIPRAMINE Ki = 94.0 nM 7.03
CHEMBL74766 Ki = 99.0 nM 7.00
CHEMBL72611 Ki = 110.0 nM 6.96
CHEMBL76281 Ki = 4610.0 nM 5.34
CHEMBL73783 Ki > 10000.0 nM -
CHEMBL75207 Ki > 10000.0 nM -