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Assay Detail

CHEMBL747321

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Functional
In Vitro 5-HT3 agonist activity on the [14C]guanidinium accumulation in NG 108-15 cells.
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type NG108-15
Confidence 1 — Organism
Curated By Intermediate

Target

NG108-15 (CHEMBL613828)
Type CELL-LINE
Organism Murinae

Publication

Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.
Prunier H, Rault S, Lancelot JC, Robba M, Renard P, Delagrange P, Pfeiffer B, Caignard DH, Misslin R, Guardiola-Lemaitre B, Hamon M.
J Med Chem (1997) 40 : 1808 -1819
PubMed 9191957 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 7.33 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54720 1 7.96
CHEMBL53416 1 7.75
CHEMBL53573 1 7.50
CHEMBL299634 1 7.28
CHEMBL53662 1 6.98
CHEMBL39 SEROTONIN 3.0 1 6.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54720 EC50 = 11.0 nM 7.96
CHEMBL53416 EC50 = 18.0 nM 7.75
CHEMBL53573 EC50 = 32.0 nM 7.50
CHEMBL299634 EC50 = 52.0 nM 7.28
CHEMBL53662 EC50 = 104.0 nM 6.98
CHEMBL39 SEROTONIN EC50 = 293.0 nM 6.53