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Assay Detail

CHEMBL2184351

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

Functional
Antagonist activity at human 5HT4ER expressed in CHO cells assessed as reduction in cAMP levels
6
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 4 (CHEMBL1875)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and pharmacological profile of new 1H-indazole-3-carboxamide and 2H-pyrrolo[3,4-c]quinoline derivatives as selective serotonin 4 receptor ligands.
Furlotti G, Alisi MA, Apicella C, Capezzone de Joannon A, Cazzolla N, Costi R, Cuzzucoli Crucitti G, Garrone B, Iacovo A, Magarò G, Mangano G, Miele G, Ombrato R, Pescatori L, Polenzani L, Rosi F, Vitiello M, Di Santo R.
J Med Chem (2012) 55 : 9446 -9466
PubMed 23043420 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kb 3 - -
IC50 3 8.75 9.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL33884 2 9.68
CHEMBL2179674 2 8.55
CHEMBL2179707 2 8.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL33884 IC50 = 0.21 nM 9.68
CHEMBL2179674 IC50 = 2.8 nM 8.55
CHEMBL2179707 IC50 = 9.8 nM 8.01
CHEMBL33884 Kb = 0.03 nM -
CHEMBL2179674 Kb = 0.41 nM -
CHEMBL2179707 Kb = 1.4 nM -