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Assay Detail

CHEMBL617698

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

Binding
Inhibition of [3H]BRL-43694 binding to 5-hydroxytryptamine 3 receptor of rat cortical homogenate.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure.
Campiani G, Cappelli A, Nacci V, Anzini M, Vomero S, Hamon M, Cagnotto A, Fracasso C, Uboldi C, Caccia S, Consolo S, Mennini T.
J Med Chem (1997) 40 : 3670 -3678
PubMed 9357534 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.84 9.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL327197 1 9.43
CHEMBL124886 1 9.36
CHEMBL341474 1 9.09
CHEMBL331304 1 8.41
CHEMBL120216 1 8.27
CHEMBL18772 QUIPAZINE 2.0 1 8.21
CHEMBL122835 1 8.05
CHEMBL120215 1 8.02
CHEMBL121076 1 7.96
CHEMBL123137 1 7.66
CHEMBL121155 1 7.66
CHEMBL121687 1 7.55
CHEMBL421059 1 7.29
CHEMBL332328 1 7.09
CHEMBL126041 1 7.06
CHEMBL39 SEROTONIN 3.0 1 6.14
CHEMBL266591 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL327197 IC50 = 0.37 nM 9.43
CHEMBL124886 IC50 = 0.44 nM 9.36
CHEMBL341474 IC50 = 0.81 nM 9.09
CHEMBL331304 IC50 = 3.9 nM 8.41
CHEMBL120216 IC50 = 5.4 nM 8.27
CHEMBL18772 QUIPAZINE IC50 = 6.2 nM 8.21
CHEMBL122835 IC50 = 9.0 nM 8.05
CHEMBL120215 IC50 = 9.5 nM 8.02
CHEMBL121076 IC50 = 11.0 nM 7.96
CHEMBL123137 IC50 = 22.0 nM 7.66
CHEMBL121155 IC50 = 22.0 nM 7.66
CHEMBL121687 IC50 = 28.0 nM 7.55
CHEMBL421059 IC50 = 51.0 nM 7.29
CHEMBL332328 IC50 = 82.0 nM 7.09
CHEMBL126041 IC50 = 88.0 nM 7.06
CHEMBL39 SEROTONIN IC50 = 727.0 nM 6.14
CHEMBL266591 IC50 = 779.0 nM 6.11