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Assay Detail

CHEMBL4013762

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

Binding
Agonist activity at tTA containing TEV cleavage site-fused 5-HT2C-INI receptor isoform (unknown origin) expressed in TEV-fused beta-arrestin2 expressing HEK cells assessed as induction of beta-arrestin2 recruitment after 20 hrs by Tango assay
11
Total Activities
6
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

Discovery of N-Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications.
Zhang G, Cheng J, McCorvy JD, Lorello PJ, Caldarone BJ, Roth BL, Kozikowski AP.
J Med Chem (2017) 60 : 6273 -6288
PubMed 28657744 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 7.60 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4091672 2 7.96
CHEMBL39 SEROTONIN 3.0 2 7.82
CHEMBL4063893 2 7.64
CHEMBL360328 LORCASERIN 4.0 2 7.40
CHEMBL4072722 2 7.16
CHEMBL4101194 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4091672 EC50 = 10.96 nM 7.96
CHEMBL4091672 EC50 = 11.0 nM 7.96
CHEMBL39 SEROTONIN EC50 = 15.14 nM 7.82
CHEMBL39 SEROTONIN EC50 = 15.0 nM 7.82
CHEMBL4063893 EC50 = 22.91 nM 7.64
CHEMBL4063893 EC50 = 22.7 nM 7.64
CHEMBL360328 LORCASERIN EC50 = 39.81 nM 7.40
CHEMBL360328 LORCASERIN EC50 = 40.0 nM 7.40
CHEMBL4072722 EC50 = 69.18 nM 7.16
CHEMBL4072722 EC50 = 70.0 nM 7.16
CHEMBL4101194 EC50 > 1000.0 nM -