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Assay Detail

CHEMBL4276583

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

Binding
Displacement of [3H]-mepyramine from histamine H1 receptor in guinea pig cerebellum homogenates incubated for 60 mins by liquid scintillation counting
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Cerebellum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H1 receptor (CHEMBL3943)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Synthesis and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
Cao X, Zhang Y, Chen Y, Qiu Y, Yu M, Xu X, Liu X, Liu BF, Zhang L, Zhang G.
J Med Chem (2018) 61 : 10017 -10039
PubMed 30383372 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.65 7.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4290311 1 7.36
CHEMBL85 RISPERIDONE 4.0 1 7.33
CHEMBL4294799 1 6.47
CHEMBL4289498 1 6.38
CHEMBL4293999 1 6.20
CHEMBL4283548 1 6.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4290311 Ki = 43.5 nM 7.36
CHEMBL85 RISPERIDONE Ki = 46.2 nM 7.33
CHEMBL4294799 Ki = 339.0 nM 6.47
CHEMBL4289498 Ki = 421.0 nM 6.38
CHEMBL4293999 Ki = 630.3 nM 6.20
CHEMBL4283548 Ki = 711.7 nM 6.15