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Assay Detail

CHEMBL2015860

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

Binding
Displacement of [3H]granisetron from 5HT3 receptor in Wistar rat cortical membranes by liquid scintillation spectrometry
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 3A (CHEMBL2411)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Bivalent Ligands for the Serotonin 5-HT3 Receptor.
Cappelli A, Manini M, Paolino M, Gallelli A, Anzini M, Mennuni L, Del Cadia M, De Rienzo F, Menziani MC, Vomero S.
ACS Med Chem Lett (2011) 2 : 571 -576
PubMed 24900351 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.37 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2011470 1 8.57
CHEMBL195241 1 8.25
CHEMBL2011586 1 8.11
CHEMBL2011588 1 7.82
CHEMBL2011596 1 7.75
CHEMBL2011591 1 7.58
CHEMBL2011587 1 7.57
CHEMBL2011469 1 7.55
CHEMBL2011471 1 7.17
CHEMBL2011590 1 7.16
CHEMBL2011589 1 7.15
CHEMBL2011600 1 7.15
CHEMBL2011599 1 7.05
CHEMBL2011593 1 6.97
CHEMBL2011597 1 6.90
CHEMBL2011598 1 6.88
CHEMBL2011592 1 6.85
CHEMBL2011594 1 6.81
CHEMBL2011595 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2011470 Ki = 2.7 nM 8.57
CHEMBL195241 Ki = 5.6 nM 8.25
CHEMBL2011586 Ki = 7.7 nM 8.11
CHEMBL2011588 Ki = 15.0 nM 7.82
CHEMBL2011596 Ki = 18.0 nM 7.75
CHEMBL2011591 Ki = 26.0 nM 7.58
CHEMBL2011587 Ki = 27.0 nM 7.57
CHEMBL2011469 Ki = 28.0 nM 7.55
CHEMBL2011471 Ki = 67.0 nM 7.17
CHEMBL2011590 Ki = 69.0 nM 7.16
CHEMBL2011589 Ki = 71.0 nM 7.15
CHEMBL2011600 Ki = 71.0 nM 7.15
CHEMBL2011599 Ki = 89.0 nM 7.05
CHEMBL2011593 Ki = 106.0 nM 6.97
CHEMBL2011597 Ki = 127.0 nM 6.90
CHEMBL2011598 Ki = 132.0 nM 6.88
CHEMBL2011592 Ki = 141.0 nM 6.85
CHEMBL2011594 Ki = 154.0 nM 6.81
CHEMBL2011595 Ki = 178.0 nM 6.75