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Assay Detail

CHEMBL991391

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

Binding
Displacement of [3H]mesulergine from 5HT2C receptor expressed in HEK293 cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

The discovery of a selective, small molecule agonist for the MAS-related gene X1 receptor.
Wroblowski B, Wigglesworth MJ, Szekeres PG, Smith GD, Rahman SS, Nicholson NH, Muir AI, Hall A, Heer JP, Garland SL, Coates WJ.
J Med Chem (2009) 52 : 818 -825
PubMed 19146417 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.76 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL458002 1 8.41
CHEMBL458001 1 7.52
CHEMBL458220 1 6.52
CHEMBL474473 1 5.81
CHEMBL477008 1 5.55
CHEMBL474474 1 -
CHEMBL475965 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL458002 Ki = 3.89 nM 8.41
CHEMBL458001 Ki = 30.2 nM 7.52
CHEMBL458220 Ki = 302.0 nM 6.52
CHEMBL474473 Ki = 1548.82 nM 5.81
CHEMBL477008 Ki = 2818.38 nM 5.55
CHEMBL474474 Ki > 6025.6 nM -
CHEMBL475965 Ki > 10000.0 nM -