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Assay Detail

CHEMBL3225632

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

Binding
Binding affinity to H1 histamine receptor (unknown origin) by PDSP assay
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

The synthesis and receptor binding affinities of DDD-016, a novel, potential, atypical antipsychotic
Bandyopadhyaya A, Rajagopalan DR, Rath NP, Herrold A, Rajagopalan R, Napier TC, Tedford CE, Rajagopalan P
Medchemcomm (2012) 3 : 580 -583
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.75 8.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3217984 1 8.50
CHEMBL715 OLANZAPINE 4.0 1 8.00
CHEMBL42 CLOZAPINE 4.0 1 8.00
CHEMBL716 QUETIAPINE 4.0 1 8.00
CHEMBL1112 ARIPIPRAZOLE 4.0 1 7.00
CHEMBL85 RISPERIDONE 4.0 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3217984 Ki = 3.162 nM 8.50
CHEMBL715 OLANZAPINE Ki = 10.0 nM 8.00
CHEMBL42 CLOZAPINE Ki = 10.0 nM 8.00
CHEMBL716 QUETIAPINE Ki = 10.0 nM 8.00
CHEMBL1112 ARIPIPRAZOLE Ki = 100.0 nM 7.00
CHEMBL85 RISPERIDONE Ki = 100.0 nM 7.00