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Assay Detail

CHEMBL4677479

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Binding
Binding affinity to H1 histamine receptor (unknown origin)
6
Total Activities
6
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

Histamine H1 receptor (CHEMBL231)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of novel antipsychotic trans-4-(2-(1,2,4,5-tetrahydro-3H-benzo[d]azepin-3-yl)ethyl)cyclohexan-1-amine derivatives targeting dopamine/serotonin receptor subtypes.
Xu JW,Qi YL,Wu JW,Yuan RX,Chen XW,Li JQ
Bioorg Med Chem Lett (2021) 31 : 127681 -127681
PubMed 33189775 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.89 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3187365 ASENAPINE 4.0 1 9.00
CHEMBL715 OLANZAPINE 4.0 1 8.15
CHEMBL716 QUETIAPINE 4.0 1 7.96
CHEMBL85 RISPERIDONE 4.0 1 7.70
CHEMBL708 ZIPRASIDONE 4.0 1 7.30
CHEMBL1112 ARIPIPRAZOLE 4.0 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3187365 ASENAPINE Ki = 1.0 nM 9.00
CHEMBL715 OLANZAPINE Ki = 7.0 nM 8.15
CHEMBL716 QUETIAPINE Ki = 11.0 nM 7.96
CHEMBL85 RISPERIDONE Ki = 20.0 nM 7.70
CHEMBL708 ZIPRASIDONE Ki = 50.0 nM 7.30
CHEMBL1112 ARIPIPRAZOLE Ki = 61.0 nM 7.21