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Assay Detail

CHEMBL1648628

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

Functional
Partial agonist activity at human 5HT3A receptor expressed in HEK293 cells assessed as decrease in 10 uM 5-chloroindole-induced increase in intracellular calcium release
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 3A (CHEMBL1899)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome.
Manning DD, Cioffi CL, Usyatinsky A, Fitzpatrick K, Masih L, Guo C, Zhang Z, Choo SH, Sikkander MI, Ryan KN, Naginskaya J, Hassler C, Dobritsa S, Wierschke JD, Earley WG, Butler AS, Brady CA, Barnes NM, Cohen ML, Guzzo PR.
Bioorg Med Chem Lett (2011) 21 : 58 -61
PubMed 21146988 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 7.68 8.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1643883 1 8.16
CHEMBL1643880 PUMOSETRAG 2.0 1 8.04
CHEMBL39 SEROTONIN 3.0 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1643883 EC50 = 6.9 nM 8.16
CHEMBL1643880 PUMOSETRAG EC50 = 9.2 nM 8.04
CHEMBL39 SEROTONIN EC50 = 141.0 nM 6.85