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Assay Detail

CHEMBL620587

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

Binding
The binding affinity was measured for 5-hydroxytryptamine 3 receptor on NG 108-15 cell line of mouse neuroblastoma-glioma cells in presence of [3H]5 radioligand (in vitro)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type NG 108-15
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Serotonin 3 receptor (5HT3) (CHEMBL2111333)
Type PROTEIN FAMILY
Organism Mus musculus

Publication

Synthesis, in vitro binding profile, and central nervous system penetrability of the highly potent 5-HT3 receptor antagonist [3H]-4-(2-methoxyphenyl)-2-[4(5)-methyl-5(4)-imidazolylmethyl]thiazole.
Rosen T, Seeger TF, McLean S, Nagel AA, Ives JL, Guarino KJ, Bryce D, Furman J, Roth RW, Chalabi PM.
J Med Chem (1990) 33 : 3020 -3023
PubMed 2231600 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.45 8.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18041 ZACOPRIDE 2.0 1 8.88
CHEMBL56564 TROPISETRON 3.0 1 8.42
CHEMBL18772 QUIPAZINE 2.0 1 8.06
CHEMBL46 ONDANSETRON 4.0 1 7.92
CHEMBL6437 MIANSERIN 4.0 1 6.60
CHEMBL39 SEROTONIN 3.0 1 6.44
CHEMBL266591 1 5.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18041 ZACOPRIDE Ki = 1.32 nM 8.88
CHEMBL56564 TROPISETRON Ki = 3.8 nM 8.42
CHEMBL18772 QUIPAZINE Ki = 8.67 nM 8.06
CHEMBL46 ONDANSETRON Ki = 12.0 nM 7.92
CHEMBL6437 MIANSERIN Ki = 252.0 nM 6.60
CHEMBL39 SEROTONIN Ki = 361.0 nM 6.44
CHEMBL266591 Ki = 1430.0 nM 5.84