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Assay Detail

CHEMBL618149

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

Binding
Binding affinity towards 5-hydroxytryptamine 3 receptor by displacement of [3H]2 in Neuroblastoma-Glioma NG-108-15 cells
7
Total Activities
7
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

Thiazole as a carbonyl bioisostere. A novel class of highly potent and selective 5-HT3 receptor antagonists.
Rosen T, Nagel AA, Rizzi JP, Ives JL, Daffeh JB, Ganong AH, Guarino K, Heym J, McLean S, Nowakowski JT.
J Med Chem (1990) 33 : 2715 -2720
PubMed 2213824 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 8.59 9.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93919 1 9.38
CHEMBL421747 1 9.00
CHEMBL38465 1 8.74
CHEMBL329179 1 8.71
CHEMBL56564 TROPISETRON 3.0 1 8.57
CHEMBL290938 1 7.92
CHEMBL46 ONDANSETRON 4.0 1 7.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93919 Ki = 0.42 nM 9.38
CHEMBL421747 Ki = 1.0 nM 9.00
CHEMBL38465 Ki = 1.8 nM 8.74
CHEMBL329179 Ki = 1.94 nM 8.71
CHEMBL56564 TROPISETRON Ki = 2.7 nM 8.57
CHEMBL290938 Ki = 12.0 nM 7.92
CHEMBL46 ONDANSETRON Ki = 16.2 nM 7.79