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Assay Detail

CHEMBL1048660

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

Binding
Displacement of [3H]Mesulergine from human recombinant 5HT2C receptor expressed in CHO-K1 cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2C (CHEMBL225)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological activity of 5-styryl and 5-phenethyl-substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles.
Ivachtchenko AV, Frolov EB, Mitkin OD, Tkachenko SE, Okun IM, Khvat AV.
Bioorg Med Chem Lett (2010) 20 : 78 -82
PubMed 19945877 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.54 9.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL605405 1 9.32
CHEMBL592752 MARITUPIRDINE 2.0 1 8.92
CHEMBL605081 1 8.80
CHEMBL589390 LATREPIRDINE 3.0 1 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL605405 Ki = 0.4786 nM 9.32
CHEMBL592752 MARITUPIRDINE Ki = 1.202 nM 8.92
CHEMBL605081 Ki = 1.585 nM 8.80
CHEMBL589390 LATREPIRDINE Ki = 75.86 nM 7.12