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Assay Detail

CHEMBL838604

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

Functional
Antagonism of 2-methyl-5-HT effect on 5-hydroxytryptamine 3 receptor in isolated guinea pig ileum
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Ileum
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Microwave assisted synthesis of 2-(4-substituted piperazin-1-yl)-1,8-naphthyridine-3-carbonitrile as a new class of serotonin 5-HT3 receptor antagonists.
Mahesh R, Perumal RV, Pandi PV.
Bioorg Med Chem Lett (2004) 14 : 5179 -5181
PubMed 15380223 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 13 6.32 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL364128 1 8.20
CHEMBL184379 1 7.40
CHEMBL185472 1 7.10
CHEMBL46 ONDANSETRON 4.0 1 6.90
CHEMBL366109 1 6.50
CHEMBL186775 1 6.00
CHEMBL186532 1 5.70
CHEMBL187181 1 5.40
CHEMBL186813 1 5.10
CHEMBL184511 1 4.90
CHEMBL185458 1 -
CHEMBL184650 1 -
CHEMBL184241 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL364128 Kd = 6.31 nM 8.20
CHEMBL184379 Kd = 39.81 nM 7.40
CHEMBL185472 Kd = 79.43 nM 7.10
CHEMBL46 ONDANSETRON Kd = 125.89 nM 6.90
CHEMBL366109 Kd = 316.23 nM 6.50
CHEMBL186775 Kd = 1000.0 nM 6.00
CHEMBL186532 Kd = 1995.26 nM 5.70
CHEMBL187181 Kd = 3981.07 nM 5.40
CHEMBL186813 Kd = 7943.28 nM 5.10
CHEMBL184511 Kd = 12589.25 nM 4.90
CHEMBL185458 Kd = 158489.32 nM -
CHEMBL184650 Kd = 1258925.41 nM -
CHEMBL184241 Kd = 125892.54 nM -