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Assay Detail

CHEMBL3095677

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

Binding
Binding affinity to 5-HT2A receptor (unknown origin)
3
Total Activities
3
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 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of new carbonyl guanidine derivatives as novel dual 5-HT2B and 5-HT7 receptor antagonists.
Moritomo A, Yamada H, Watanabe T, Itahana H, Akuzawa S, Okada M, Ohta M.
Bioorg Med Chem (2013) 21 : 7841 -7852
PubMed 24189186 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.06 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL294951 PIZOTYLINE 2.0 1 8.12
CHEMBL3092753 1 6.00
CHEMBL3092759 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL294951 PIZOTYLINE Ki = 7.5 nM 8.12
CHEMBL3092753 Ki = 1000.0 nM 6.00
CHEMBL3092759 Ki > 1000.0 nM -