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Assay Detail

CHEMBL964233

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Binding
Binding affinity at 5HT3 receptor
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 3A (CHEMBL1899)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel antagonists of serotonin-4 receptors: synthesis and biological evaluation of pyrrolothienopyrazines.
Lemaître S, Lepailleur A, Bureau R, Butt-Gueulle S, Lelong-Boulouard V, Duchatelle P, Boulouard M, Dumuis A, Daveu C, Lezoualc'h F, Pfeiffer B, Dauphin F, Rault S.
Bioorg Med Chem (2009) 17 : 2607 -2622
PubMed 19261477 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 6.64 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56564 TROPISETRON 3.0 1 8.55
CHEMBL287045 1 6.90
CHEMBL68131 1 6.80
CHEMBL472219 1 6.60
CHEMBL3084582 1 6.50
CHEMBL83954 1 5.70
CHEMBL117287 PRUCALOPRIDE 4.0 1 5.40
CHEMBL33884 1 -
CHEMBL356359 PIBOSEROD 2.0 1 -
CHEMBL76370 TEGASEROD 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56564 TROPISETRON Ki = 2.818 nM 8.55
CHEMBL287045 Ki = 125.89 nM 6.90
CHEMBL68131 Ki = 158.49 nM 6.80
CHEMBL472219 Ki = 251.19 nM 6.60
CHEMBL3084582 Ki = 316.23 nM 6.50
CHEMBL83954 Ki = 1995.26 nM 5.70
CHEMBL117287 PRUCALOPRIDE Ki = 3981.07 nM 5.40
CHEMBL33884 Ki > 10000.0 nM -
CHEMBL356359 PIBOSEROD Ki > 1000.0 nM -
CHEMBL76370 TEGASEROD Ki > 10000.0 nM -