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Assay Detail

CHEMBL3243869

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

Functional
Antagonist activity at human recombinant 5HT2A receptor expressed in HEK293a cells assessed as inhibition of serotonin-induced increase in calcium fluorescence
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.
Li P, Zhang Q, Robichaud AJ, Lee T, Tomesch J, Yao W, Beard JD, Snyder GL, Zhu H, Peng Y, Hendrick JP, Vanover KE, Davis RE, Mates S, Wennogle LP.
J Med Chem (2014) 57 : 2670 -2682
PubMed 24559051 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.15 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3233142 LUMATEPERONE TOSYLATE 4.0 1 8.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3233142 LUMATEPERONE TOSYLATE IC50 = 7.0 nM 8.15