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Assay Detail

CHEMBL1648623

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

Binding
Binding affinity to human 5HT3A receptor
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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
Ki 17 8.71 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1643895 RAMOSETRON 4.0 1 10.22
CHEMBL1110 ALOSETRON 4.0 1 9.30
CHEMBL1643884 1 9.15
CHEMBL1643894 1 9.15
CHEMBL1643893 1 9.05
CHEMBL1643887 1 8.80
CHEMBL1643883 1 8.77
CHEMBL1643886 1 8.70
CHEMBL1643885 1 8.70
CHEMBL1643889 1 8.64
CHEMBL1641625 1 8.62
CHEMBL1643888 1 8.44
CHEMBL1643881 1 8.36
CHEMBL1643882 1 8.31
CHEMBL1643890 1 8.15
CHEMBL1643892 1 8.10
CHEMBL1643891 1 7.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1643895 RAMOSETRON Ki = 0.06 nM 10.22
CHEMBL1110 ALOSETRON Ki = 0.5 nM 9.30
CHEMBL1643884 Ki = 0.7 nM 9.15
CHEMBL1643894 Ki = 0.7 nM 9.15
CHEMBL1643893 Ki = 0.9 nM 9.05
CHEMBL1643887 Ki = 1.6 nM 8.80
CHEMBL1643883 Ki = 1.7 nM 8.77
CHEMBL1643886 Ki = 2.0 nM 8.70
CHEMBL1643885 Ki = 2.0 nM 8.70
CHEMBL1643889 Ki = 2.3 nM 8.64
CHEMBL1641625 Ki = 2.4 nM 8.62
CHEMBL1643888 Ki = 3.6 nM 8.44
CHEMBL1643881 Ki = 4.4 nM 8.36
CHEMBL1643882 Ki = 4.9 nM 8.31
CHEMBL1643890 Ki = 7.1 nM 8.15
CHEMBL1643892 Ki = 7.9 nM 8.10
CHEMBL1643891 Ki = 23.4 nM 7.63