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Assay Detail

CHEMBL3294608

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

Binding
Displacement of [3H]5-HT from 5-HT2C receptor (unknown origin) expressed in hamster AV12 cells
4
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type AV12
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Novel aza-analogous ergoline derived scaffolds as potent serotonin 5-HT₆ and dopamine D₂ receptor ligands.
Krogsgaard-Larsen N, Jensen AA, Schrøder TJ, Christoffersen CT, Kehler J.
J Med Chem (2014) 57 : 5823 -5828
PubMed 24878269 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.36 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3286580 IDALOPIRDINE 3.0 2 6.60
CHEMBL431298 2 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3286580 IDALOPIRDINE Ki = 250.0 nM 6.60
CHEMBL3286580 IDALOPIRDINE Ki = 251.19 nM 6.60
CHEMBL431298 Ki = 770.0 nM 6.11
CHEMBL431298 Ki = 776.25 nM 6.11