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Assay Detail

CHEMBL4397382

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

Binding
Displacement of [3H]-mesulergine from recombinant human 5HT2C receptor transiently expressed in HEKT cell membranes measured after 90 mins by microbeta scintillation counting method
1
Total Activities
1
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

Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine D<sub>3</sub> Receptor (D<sub>3</sub>R) Ligand Promiscuity across Highly Conserved Aminergic G-Protein-Coupled Receptors (GPCRs).
Reilly SW, Riad AA, Hsieh CJ, Sahlholm K, Jacome DA, Griffin S, Taylor M, Weng CC, Xu K, Kirschner N, Luedtke RR, Parry C, Malhotra S, Karanicolas J, Mach RH.
J Med Chem (2019) 62 : 5132 -5147
PubMed 31021617 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 6.80 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4083252 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4083252 Ki = 159.0 nM 6.80