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Assay Detail

CHEMBL617016

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

Binding
In vitro binding affinity to 5-hydroxytryptamine 2 receptor of rat cerebral cortex membranes using [3H]ketanserin as the radioligand
ChEMBL ↗
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Serotonin 2 (5-HT2) receptor (CHEMBL2093870) ↗
Type PROTEIN FAMILY
Organism Rattus norvegicus

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 6.76 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68094 — — 1 7.80
CHEMBL70048 — — 1 7.55
CHEMBL422587 — — 1 7.40
CHEMBL12427 — — 1 7.37
CHEMBL304167 — — 1 7.35
CHEMBL69040 — — 1 7.34
CHEMBL428494 — — 1 7.27
CHEMBL71847 — — 1 7.19
CHEMBL71165 — — 1 7.12
CHEMBL418888 — — 1 7.10
CHEMBL307686 — — 1 7.01
CHEMBL69257 — — 1 7.01
CHEMBL307101 — — 1 7.01
CHEMBL273246 — — 1 6.98
CHEMBL12702 — — 1 6.95
CHEMBL304731 — — 1 6.94
CHEMBL72008 — — 1 6.91
CHEMBL70819 — — 1 6.88
CHEMBL12846 — — 1 6.84
CHEMBL70764 — — 1 6.80
CHEMBL71390 — — 1 6.69
CHEMBL71383 — — 1 6.62
CHEMBL302766 — — 1 6.55
CHEMBL71057 — — 1 6.54
CHEMBL303166 — — 1 6.45
CHEMBL307352 — — 1 6.43
CHEMBL302093 — — 1 6.35
CHEMBL305526 — — 1 6.28
CHEMBL71225 — — 1 6.27
CHEMBL71224 — — 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68094 — Ki = 15.85 nM 7.80
CHEMBL70048 — Ki = 28.18 nM 7.55
CHEMBL422587 — Ki = 39.81 nM 7.40
CHEMBL12427 — Ki = 42.66 nM 7.37
CHEMBL304167 — Ki = 44.67 nM 7.35
CHEMBL69040 — Ki = 45.71 nM 7.34
CHEMBL428494 — Ki = 53.7 nM 7.27
CHEMBL71847 — Ki = 64.57 nM 7.19
CHEMBL71165 — Ki = 75.86 nM 7.12
CHEMBL418888 — Ki = 79.43 nM 7.10
CHEMBL69257 — Ki = 97.72 nM 7.01
CHEMBL307101 — Ki = 97.72 nM 7.01
CHEMBL307686 — Ki = 97.72 nM 7.01
CHEMBL273246 — Ki = 104.71 nM 6.98
CHEMBL12702 — Ki = 112.2 nM 6.95
CHEMBL304731 — Ki = 114.82 nM 6.94
CHEMBL72008 — Ki = 123.03 nM 6.91
CHEMBL70819 — Ki = 131.83 nM 6.88
CHEMBL12846 — Ki = 144.54 nM 6.84
CHEMBL70764 — Ki = 158.49 nM 6.80
CHEMBL71390 — Ki = 204.17 nM 6.69
CHEMBL71383 — Ki = 239.88 nM 6.62
CHEMBL302766 — Ki = 281.84 nM 6.55
CHEMBL71057 — Ki = 288.4 nM 6.54
CHEMBL303166 — Ki = 354.81 nM 6.45
CHEMBL307352 — Ki = 371.54 nM 6.43
CHEMBL302093 — Ki = 446.68 nM 6.35
CHEMBL305526 — Ki = 524.81 nM 6.28
CHEMBL71225 — Ki = 537.03 nM 6.27
CHEMBL71224 — Ki = 575.44 nM 6.24
CHEMBL308461 — Ki = 676.08 nM 6.17
CHEMBL71959 — Ki = 758.58 nM 6.12
CHEMBL70889 — Ki = 812.83 nM 6.09
CHEMBL70869 — Ki = 891.25 nM 6.05
CHEMBL69388 — Ki = 1380.38 nM 5.86
CHEMBL302723 — Ki = 1412.54 nM 5.85
CHEMBL71170 — Ki < 1000.0 nM -
CHEMBL553794 — Ki < 1000.0 nM -
CHEMBL18840 — Ki < 1000.0 nM -
CHEMBL273890 — Ki < 1000.0 nM -