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Assay Detail

CHEMBL617704

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

Binding
Inhibition of [3H]GR-65630 binding to rat cortical membrane serotonin 3 receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Pyrazolo[1,5-a]pyridines and pyrazolo[1,5-b]pyridazines as 5ht3-antagonists
Bondo Hansen J, Weis J, Suzdak P, Eskesen K
Bioorg Med Chem Lett (1994) 4 : 695 -698
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.26 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56564 TROPISETRON 3.0 1 8.51
CHEMBL159405 1 7.58
CHEMBL350972 1 7.55
CHEMBL355149 1 7.47
CHEMBL159821 1 7.28
CHEMBL348809 1 7.19
CHEMBL349444 1 7.14
CHEMBL162078 1 7.12
CHEMBL351714 1 6.91
CHEMBL159293 1 6.77
CHEMBL160109 1 6.37
CHEMBL161411 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56564 TROPISETRON IC50 = 3.1 nM 8.51
CHEMBL159405 IC50 = 26.0 nM 7.58
CHEMBL350972 IC50 = 28.0 nM 7.55
CHEMBL355149 IC50 = 34.0 nM 7.47
CHEMBL159821 IC50 = 52.0 nM 7.28
CHEMBL348809 IC50 = 64.0 nM 7.19
CHEMBL349444 IC50 = 72.0 nM 7.14
CHEMBL162078 IC50 = 75.0 nM 7.12
CHEMBL351714 IC50 = 122.0 nM 6.91
CHEMBL159293 IC50 = 170.0 nM 6.77
CHEMBL160109 IC50 = 429.0 nM 6.37
CHEMBL161411 IC50 > 300.0 nM -