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Assay Detail

CHEMBL1033065

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Functional
Antagonist activity at dopamine D2 receptor
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(2) dopamine receptor (CHEMBL217)
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
IC50 5 7.73 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3084515 1 8.72
CHEMBL445102 1 8.35
CHEMBL3084512 1 7.58
CHEMBL3084502 1 7.32
CHEMBL3084503 1 6.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3084515 IC50 = 1.92 nM 8.72
CHEMBL445102 IC50 = 4.46 nM 8.35
CHEMBL3084512 IC50 = 26.2 nM 7.58
CHEMBL3084502 IC50 = 48.3 nM 7.32
CHEMBL3084503 IC50 = 210.0 nM 6.68