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Assay Detail

CHEMBL958366

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

Binding
Displacement of [3H]mesulergine from 5HT2C receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action.
Cho SJ, Jensen NH, Kurome T, Kadari S, Manzano ML, Malberg JE, Caldarone B, Roth BL, Kozikowski AP.
J Med Chem (2009) 52 : 1885 -1902
PubMed 19284718 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.76 7.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL467736 1 7.18
CHEMBL492916 1 6.91
CHEMBL451232 1 6.69
CHEMBL493130 1 6.62
CHEMBL360328 LORCASERIN 4.0 1 6.59
CHEMBL445747 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL467736 Ki = 66.0 nM 7.18
CHEMBL492916 Ki = 124.0 nM 6.91
CHEMBL451232 Ki = 203.0 nM 6.69
CHEMBL493130 Ki = 242.0 nM 6.62
CHEMBL360328 LORCASERIN Ki = 257.0 nM 6.59
CHEMBL445747 Ki = 268.0 nM 6.57