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Assay Detail

CHEMBL618165

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

Binding
Binding affinity to human recombinant 5-hydroxytryptamine 7 receptor in mammalian cells using [3H]5-CT as radioligand
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 7 (CHEMBL3155)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2a-[4-(Tetrahydropyridoindol-2-yl)butyl]tetrahydrobenzindole derivatives: new selective antagonists of the 5-hydroxytryptamine7 receptor.
Kikuchi C, Ando T, Watanabe T, Nagaso H, Okuno M, Hiranuma T, Koyama M.
J Med Chem (2002) 45 : 2197 -2206
PubMed 12014957 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 40 7.87 9.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18840 1 9.31
CHEMBL428494 1 8.73
CHEMBL69257 1 8.67
CHEMBL71847 1 8.63
CHEMBL12427 1 8.48
CHEMBL553794 1 8.45
CHEMBL418888 1 8.45
CHEMBL273246 1 8.42
CHEMBL12846 1 8.40
CHEMBL304731 1 8.32
CHEMBL12702 1 8.29
CHEMBL71383 1 8.24
CHEMBL302766 1 8.22
CHEMBL71225 1 8.19
CHEMBL71959 1 8.15
CHEMBL303166 1 8.10
CHEMBL422587 1 8.09
CHEMBL70889 1 8.06
CHEMBL304167 1 7.98
CHEMBL71057 1 7.91
CHEMBL307101 1 7.91
CHEMBL71224 1 7.77
CHEMBL70869 1 7.76
CHEMBL305526 1 7.72
CHEMBL71170 1 7.72
CHEMBL71390 1 7.69
CHEMBL307352 1 7.66
CHEMBL69040 1 7.62
CHEMBL70819 1 7.60
CHEMBL308461 1 7.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18840 Ki = 0.4898 nM 9.31
CHEMBL428494 Ki = 1.862 nM 8.73
CHEMBL69257 Ki = 2.138 nM 8.67
CHEMBL71847 Ki = 2.344 nM 8.63
CHEMBL12427 Ki = 3.311 nM 8.48
CHEMBL553794 Ki = 3.548 nM 8.45
CHEMBL418888 Ki = 3.548 nM 8.45
CHEMBL273246 Ki = 3.802 nM 8.42
CHEMBL12846 Ki = 3.981 nM 8.40
CHEMBL304731 Ki = 4.786 nM 8.32
CHEMBL12702 Ki = 5.129 nM 8.29
CHEMBL71383 Ki = 5.754 nM 8.24
CHEMBL302766 Ki = 6.026 nM 8.22
CHEMBL71225 Ki = 6.457 nM 8.19
CHEMBL71959 Ki = 7.079 nM 8.15
CHEMBL303166 Ki = 7.943 nM 8.10
CHEMBL422587 Ki = 8.128 nM 8.09
CHEMBL70889 Ki = 8.71 nM 8.06
CHEMBL304167 Ki = 10.47 nM 7.98
CHEMBL307101 Ki = 12.3 nM 7.91
CHEMBL71057 Ki = 12.3 nM 7.91
CHEMBL71224 Ki = 16.98 nM 7.77
CHEMBL70869 Ki = 17.38 nM 7.76
CHEMBL305526 Ki = 19.05 nM 7.72
CHEMBL71170 Ki = 19.05 nM 7.72
CHEMBL71390 Ki = 20.42 nM 7.69
CHEMBL307352 Ki = 21.88 nM 7.66
CHEMBL69040 Ki = 23.99 nM 7.62
CHEMBL70819 Ki = 25.12 nM 7.60
CHEMBL308461 Ki = 29.51 nM 7.53
CHEMBL302093 Ki = 43.65 nM 7.36
CHEMBL72008 Ki = 45.71 nM 7.34
CHEMBL307686 Ki = 72.44 nM 7.14
CHEMBL69388 Ki = 74.13 nM 7.13
CHEMBL71165 Ki = 97.72 nM 7.01
CHEMBL70048 Ki = 109.65 nM 6.96
CHEMBL302723 Ki = 147.91 nM 6.83
CHEMBL68094 Ki = 223.87 nM 6.65
CHEMBL70764 Ki = 416.87 nM 6.38
CHEMBL273890 Ki < 1000.0 nM -