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Assay Detail

CHEMBL5509700

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

Functional
Agonist activity at human 5-HT2CR expressed in HEK293 cells incubated upto 90 sec by Fluo-4 AM dye based Ca2+ imaging assay
23
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery and Structure-Activity Relationships of 2,5-Dimethoxyphenylpiperidines as Selective Serotonin 5-HT<sub>2A</sub> Receptor Agonists.
M Ro Rsted E, Jensen AA, Smits G, Frydenvang K, Kristensen JL.
J Med Chem (2024) 67 : 7224 -7244
PubMed 38648420 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 23 5.12 5.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39 SEROTONIN 3.0 1 5.58
CHEMBL292821 1 5.39
CHEMBL5527952 1 5.28
CHEMBL5532283 2 4.75
CHEMBL5557122 1 -
CHEMBL5558376 1 -
CHEMBL5556242 1 -
CHEMBL5565114 1 -
CHEMBL5555473 1 -
CHEMBL5558409 2 -
CHEMBL5537031 1 -
CHEMBL5555278 2 -
CHEMBL5517964 2 -
CHEMBL5517969 1 -
CHEMBL5537074 1 -
CHEMBL5517765 1 -
CHEMBL5556762 1 -
CHEMBL5557170 1 -
CHEMBL5532020 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39 SEROTONIN EC50 = 2600.0 nM 5.58
CHEMBL292821 EC50 = 4100.0 nM 5.39
CHEMBL5527952 EC50 = 5200.0 nM 5.28
CHEMBL5532283 EC50 = 18000.0 nM 4.75
CHEMBL5532283 EC50 = 26000.0 nM 4.58
CHEMBL5557122 EC50 = 1800000.0 nM -
CHEMBL5558376 EC50 = 2800000.0 nM -
CHEMBL5556242 EC50 ~ 10000000.0 nM -
CHEMBL5565114 EC50 = 860000.0 nM -
CHEMBL5555473 EC50 = 1200000.0 nM -
CHEMBL5558409 EC50 = 380000.0 nM -
CHEMBL5558409 EC50 = 640000.0 nM -
CHEMBL5537031 EC50 = 1600000.0 nM -
CHEMBL5555278 EC50 = 510000.0 nM -
CHEMBL5555278 EC50 = 2300000.0 nM -
CHEMBL5517964 EC50 = 570000.0 nM -
CHEMBL5517964 EC50 = 780000.0 nM -
CHEMBL5517969 EC50 = 2300000.0 nM -
CHEMBL5537074 EC50 = 920000.0 nM -
CHEMBL5517765 EC50 = 1400000.0 nM -
CHEMBL5556762 EC50 = 1400000.0 nM -
CHEMBL5557170 EC50 = 2700000.0 nM -
CHEMBL5532020 EC50 = 290000.0 nM -