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Assay Detail

CHEMBL1033061

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

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

Assay Information

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

Target

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

Publication

Structure-activity relationships for a novel series of dopamine D2-like receptor ligands based on N-substituted 3-aryl-8-azabicyclo[3.2.1]octan-3-ol.
Paul NM, Taylor M, Kumar R, Deschamps JR, Luedtke RR, Newman AH.
J Med Chem (2008) 51 : 6095 -6109
PubMed 18774793 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.19 7.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3084512 1 7.15
CHEMBL3084515 1 6.77
CHEMBL445102 1 6.16
CHEMBL3084503 1 5.55
CHEMBL3084502 1 5.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3084512 Ki = 70.1 nM 7.15
CHEMBL3084515 Ki = 171.0 nM 6.77
CHEMBL445102 Ki = 695.0 nM 6.16
CHEMBL3084503 Ki = 2800.0 nM 5.55
CHEMBL3084502 Ki = 4770.0 nM 5.32