Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4260786

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

Binding
Displacement of [3H]Mesulergine from human 5-HT2C receptor expressed in HEK293FlpIN cells by radioligand binding assay
8
Total Activities
8
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 2C (CHEMBL225)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Analogs of penfluridol as chemotherapeutic agents with reduced central nervous system activity.
Ashraf-Uz-Zaman M, Sajib MS, Cucullo L, Mikelis CM, German NA.
Bioorg Med Chem Lett (2018) 28 : 3652 -3657
PubMed 30389290 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 5.92 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4291048 1 6.40
CHEMBL4293307 1 6.13
CHEMBL47050 PENFLURIDOL 2.0 1 6.05
CHEMBL4278465 1 5.95
CHEMBL4287623 1 5.79
CHEMBL1644978 1 5.77
CHEMBL1644980 1 5.67
CHEMBL4282702 1 5.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4291048 Ki = 402.0 nM 6.40
CHEMBL4293307 Ki = 740.0 nM 6.13
CHEMBL47050 PENFLURIDOL Ki = 881.0 nM 6.05
CHEMBL4278465 Ki = 1126.0 nM 5.95
CHEMBL4287623 Ki = 1603.0 nM 5.79
CHEMBL1644978 Ki = 1712.0 nM 5.77
CHEMBL1644980 Ki = 2131.0 nM 5.67
CHEMBL4282702 Ki = 2548.0 nM 5.59