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Assay Detail

CHEMBL915407

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

Binding
Displacement of [3H]granisetron from 5HT3 receptor in Wistar rat cerebral cortex synaptosomal membranes
15
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
Subcellular Membrane
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Serotonin 3 (5-HT3) receptor (CHEMBL2094116)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Synthesis of tropeines and allosteric modulation of ionotropic glycine receptors.
Maksay G, Nemes P, Bíró T.
J Med Chem (2004) 47 : 6384 -6391
PubMed 15566307 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.59 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3085040 1 8.14
CHEMBL3085041 1 7.25
CHEMBL3085049 1 7.17
CHEMBL3085048 1 7.15
CHEMBL3085045 1 6.74
CHEMBL3085052 1 6.64
CHEMBL3085053 1 6.58
CHEMBL1947052 2 6.53
CHEMBL3085055 1 6.24
CHEMBL3085054 1 6.16
CHEMBL3085042 1 6.14
CHEMBL1947049 2 6.00
CHEMBL3085046 1 5.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3085040 IC50 = 7.178 nM 8.14
CHEMBL3085041 IC50 = 56.23 nM 7.25
CHEMBL3085049 IC50 = 67.92 nM 7.17
CHEMBL3085048 IC50 = 70.96 nM 7.15
CHEMBL3085045 IC50 = 182.39 nM 6.74
CHEMBL3085052 IC50 = 230.67 nM 6.64
CHEMBL3085053 IC50 = 262.42 nM 6.58
CHEMBL1947052 IC50 = 298.54 nM 6.53
CHEMBL1947052 IC50 = 498.88 nM 6.30
CHEMBL3085055 IC50 = 576.77 nM 6.24
CHEMBL3085054 IC50 = 691.83 nM 6.16
CHEMBL3085042 IC50 = 716.14 nM 6.14
CHEMBL1947049 IC50 = 1004.62 nM 6.00
CHEMBL3085046 IC50 = 1051.96 nM 5.98
CHEMBL1947049 IC50 = 1563.15 nM 5.81