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Assay Detail

CHEMBL617823

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

Functional
Antagonistic activity against Serotonin 5-hydroxytryptamine 3 receptor of isolated guinea pig ileum (GPI)
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Ileum
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Serotonin 3 (5-HT3) receptor (CHEMBL2094132)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Design and synthesis of novel ligands for the 5-HT3 and the 5-HT4 receptor
Blum E, Buchheit K, Buescher H, Gamse R, Kloeppner E, Meigel H, Papageorgiou C, Waelchli R, Revesz L
Bioorg Med Chem Lett (1992) 2 : 461 -466
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 12 7.18 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL143197 1 8.80
CHEMBL56564 TROPISETRON 3.0 1 7.90
CHEMBL434999 1 7.90
CHEMBL142687 1 7.70
CHEMBL2448558 1 7.60
CHEMBL1729 CISAPRIDE 4.0 1 7.20
CHEMBL356567 1 7.20
CHEMBL356287 1 6.80
CHEMBL143871 1 6.70
CHEMBL337591 1 6.00
CHEMBL86 METOCLOPRAMIDE 4.0 1 5.20
CHEMBL46 ONDANSETRON 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL143197 Kd = 1.585 nM 8.80
CHEMBL56564 TROPISETRON Kd = 12.59 nM 7.90
CHEMBL434999 Kd = 12.59 nM 7.90
CHEMBL142687 Kd = 19.95 nM 7.70
CHEMBL2448558 Kd = 25.12 nM 7.60
CHEMBL1729 CISAPRIDE Kd = 63.1 nM 7.20
CHEMBL356567 Kd = 63.1 nM 7.20
CHEMBL356287 Kd = 158.49 nM 6.80
CHEMBL143871 Kd = 199.53 nM 6.70
CHEMBL337591 Kd = 1000.0 nM 6.00
CHEMBL86 METOCLOPRAMIDE Kd = 6309.57 nM 5.20
CHEMBL46 ONDANSETRON Kd = 79.43 nM -