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Assay Detail

CHEMBL858013

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Binding
Compound was measured for the inhibition of [3H]ketanserin binding to rat frontal cortex membrane (5-HT2A receptor)
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Frontal cortex
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Butyrophenone analogues in the carbazole series: synthesis and determination of affinities at D2 and 5-HT2A receptors.
Masaguer CF, Formoso E, Raviña E, Tristán H, Loza MI, Rivas E, Fontenla JA.
Bioorg Med Chem Lett (1998) 8 : 3571 -3576
PubMed 9934473 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.77 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL333174 1 8.80
CHEMBL42 CLOZAPINE 4.0 1 8.12
CHEMBL120903 1 8.04
CHEMBL54 HALOPERIDOL 4.0 1 7.70
CHEMBL121744 1 6.20
CHEMBL327038 1 -
CHEMBL118947 1 -
CHEMBL118477 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL333174 Ki = 1.585 nM 8.80
CHEMBL42 CLOZAPINE Ki = 7.586 nM 8.12
CHEMBL120903 Ki = 9.12 nM 8.04
CHEMBL54 HALOPERIDOL Ki = 19.95 nM 7.70
CHEMBL121744 Ki = 630.96 nM 6.20
CHEMBL327038 Ki < 10000.0 nM -
CHEMBL118947 Ki < 10000.0 nM -
CHEMBL118477 Ki < 10000.0 nM -