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Assay Detail

CHEMBL5359161

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

Functional
Partial agonist activity at human 5-HT2BR expressed in human Flp-In-T-REx-293 cells assessed as increase in calcium flux incubated for 60 mins followed by incubation for 30 mins in dark by Flou-4 dye based FLIPR assay
8
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Flp-In-T-REx-293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2B (CHEMBL1833)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of Spiro[chromene-2,4'-piperidine]s as Potent, Selective, and G<sub>q</sub>-Biased 5-HT<sub>2C</sub> Receptor Partial Agonists.
Jiang G, Zhang B, Zhang X, Chen F, Qin W, Chen JL, Tian S, Shui W, Ye N.
ACS Med Chem Lett (2024) 15 : 99 -106
PubMed 38229745 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 7.11 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39 SEROTONIN 3.0 2 8.92
CHEMBL5416800 2 7.20
CHEMBL5396618 2 6.33
CHEMBL4913232 2 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39 SEROTONIN EC50 = 1.19 nM 8.92
CHEMBL39 SEROTONIN EC50 = 1.259 nM 8.90
CHEMBL5416800 EC50 = 63.1 nM 7.20
CHEMBL5416800 EC50 = 68.4 nM 7.17
CHEMBL5396618 EC50 = 469.7 nM 6.33
CHEMBL5396618 EC50 = 501.19 nM 6.30
CHEMBL4913232 EC50 = 897.0 nM 6.05
CHEMBL4913232 EC50 = 1000.0 nM 6.00