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Assay Detail

CHEMBL4844560

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Functional
Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay
3
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NG108-15
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 6 (CHEMBL3371)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Design and Optimization of FPPQ, a Dual-Acting 5-HT<sub>3</sub> and 5-HT<sub>6</sub> Receptor Antagonist with Antipsychotic and Procognitive Properties.
Zajdel P, Grychowska K, Mogilski S, Kurczab R, Satała G, Bugno R, Kos T, Gołębiowska J, Malikowska-Racia N, Nikiforuk A, Chaumont-Dubel S, Bantreil X, Pawłowski M, Martinez J, Subra G, Lamaty F, Marin P, Bojarski AJ, Popik P.
J Med Chem (2021) 64 : 13279 -13298
PubMed 34467765 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.78 8.55
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1083390 INTEPIRDINE 3.0 1 8.55
CHEMBL1210710 SB-399885 1 7.01
CHEMBL4867565 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1083390 INTEPIRDINE IC50 = 2.8 nM 8.55
CHEMBL1210710 SB-399885 IC50 = 97.0 nM 7.01
CHEMBL4867565 Activity - -