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Assay Detail

CHEMBL992739

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

Binding
Binding affinity to human cloned 5HT6 receptor
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 6 (CHEMBL3371)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.
Ablordeppey SY, Altundas R, Bricker B, Zhu XY, Kumar EV, Jackson T, Khan A, Roth BL.
Bioorg Med Chem (2008) 16 : 7291 -7301
PubMed 18595716 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.63 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL715 OLANZAPINE 4.0 1 8.00
CHEMBL42 CLOZAPINE 4.0 1 7.96
CHEMBL708 ZIPRASIDONE 4.0 1 7.12
CHEMBL476108 1 6.53
CHEMBL716 QUETIAPINE 4.0 1 5.85
CHEMBL85 RISPERIDONE 4.0 1 5.70
CHEMBL54 HALOPERIDOL 4.0 1 5.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL715 OLANZAPINE Ki = 10.0 nM 8.00
CHEMBL42 CLOZAPINE Ki = 11.0 nM 7.96
CHEMBL708 ZIPRASIDONE Ki = 76.0 nM 7.12
CHEMBL476108 Ki = 295.9 nM 6.53
CHEMBL716 QUETIAPINE Ki = 1400.0 nM 5.85
CHEMBL85 RISPERIDONE Ki = 2000.0 nM 5.70
CHEMBL54 HALOPERIDOL Ki = 6000.0 nM 5.22