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Assay Detail

CHEMBL872925

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

Binding
In vitro affinity for 5-hydroxytryptamine 3 (5-HT3) receptor by displacement of [3H]BRL-43694 from rat entorhinal cortex
43
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Serotonin 3 (5-HT3) receptor (CHEMBL2094116)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Phenylimidazolidin-2-one derivatives as selective 5-HT3 receptor antagonists and refinement of the pharmacophore model for 5-HT3 receptor binding.
Heidempergher F, Pillan A, Pinciroli V, Vaghi F, Arrigoni C, Bolis G, Caccia C, Dho L, McArthur R, Varasi M.
J Med Chem (1997) 40 : 3369 -3380
PubMed 9341912 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 43 8.12 10.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1160926 1 10.42
CHEMBL285999 1 9.59
CHEMBL289469 GRANISETRON 4.0 1 9.46
CHEMBL1160920 1 9.38
CHEMBL1160932 1 9.30
CHEMBL1160929 1 9.21
CHEMBL1160927 1 9.03
CHEMBL46 ONDANSETRON 4.0 1 9.00
CHEMBL113213 1 9.00
CHEMBL1160928 1 8.80
CHEMBL56564 TROPISETRON 3.0 1 8.80
CHEMBL114100 1 8.70
CHEMBL1160930 1 8.57
CHEMBL333144 1 8.52
CHEMBL1160925 1 8.47
CHEMBL1160923 1 8.44
CHEMBL1160924 1 8.43
CHEMBL114093 1 8.40
CHEMBL1160922 1 8.40
CHEMBL114042 1 8.22
CHEMBL114101 1 8.22
CHEMBL609962 1 8.18
CHEMBL114387 1 8.10
CHEMBL1160921 1 8.07
CHEMBL1160917 1 8.01
CHEMBL111882 1 8.00
CHEMBL333398 1 7.92
CHEMBL1160919 1 7.72
CHEMBL324719 2 7.60
CHEMBL320994 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1160926 Ki = 0.038 nM 10.42
CHEMBL285999 Ki = 0.26 nM 9.59
CHEMBL289469 GRANISETRON Ki = 0.35 nM 9.46
CHEMBL1160920 Ki = 0.42 nM 9.38
CHEMBL1160932 Ki = 0.5 nM 9.30
CHEMBL1160929 Ki = 0.62 nM 9.21
CHEMBL1160927 Ki = 0.93 nM 9.03
CHEMBL46 ONDANSETRON Ki = 1.0 nM 9.00
CHEMBL113213 Ki = 1.0 nM 9.00
CHEMBL1160928 Ki = 1.6 nM 8.80
CHEMBL56564 TROPISETRON Ki = 1.57 nM 8.80
CHEMBL114100 Ki = 2.0 nM 8.70
CHEMBL1160930 Ki = 2.7 nM 8.57
CHEMBL333144 Ki = 3.0 nM 8.52
CHEMBL1160925 Ki = 3.4 nM 8.47
CHEMBL1160923 Ki = 3.6 nM 8.44
CHEMBL1160924 Ki = 3.7 nM 8.43
CHEMBL114093 Ki = 4.0 nM 8.40
CHEMBL1160922 Ki = 4.0 nM 8.40
CHEMBL114042 Ki = 6.0 nM 8.22
CHEMBL114101 Ki = 6.0 nM 8.22
CHEMBL609962 Ki = 6.6 nM 8.18
CHEMBL114387 Ki = 8.0 nM 8.10
CHEMBL1160921 Ki = 8.5 nM 8.07
CHEMBL1160917 Ki = 9.7 nM 8.01
CHEMBL111882 Ki = 10.0 nM 8.00
CHEMBL333398 Ki = 12.0 nM 7.92
CHEMBL1160919 Ki = 19.0 nM 7.72
CHEMBL324719 Ki = 25.0 nM 7.60
CHEMBL320994 Ki = 30.0 nM 7.52
CHEMBL326150 Ki = 40.0 nM 7.40
CHEMBL333834 Ki = 55.0 nM 7.26
CHEMBL115288 Ki = 67.0 nM 7.17
CHEMBL1160931 Ki = 85.0 nM 7.07
CHEMBL114921 Ki = 98.0 nM 7.01
CHEMBL112161 Ki = 190.0 nM 6.72
CHEMBL114569 Ki = 210.0 nM 6.68
CHEMBL117551 Ki = 250.0 nM 6.60
CHEMBL1160918 Ki = 290.0 nM 6.54
CHEMBL117551 Ki = 360.0 nM 6.44
CHEMBL114911 Ki = 400.0 nM 6.40
CHEMBL325283 Ki > 10000.0 nM -
CHEMBL324719 Ki > 10000.0 nM -