Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL616834

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

Binding
Binding affinity towards 5-hydroxytryptamine 1C receptor from frontal cortical regions of male Sprague-Dawley rat homogenates, using [3H]mesulergine as radioligand
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2C (CHEMBL324)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Binding of phenylalkylamine derivatives at 5-HT1C and 5-HT2 serotonin receptors: evidence for a lack of selectivity.
Glennon RA, Raghupathi R, Bartyzel P, Teitler M, Leonhardt S.
J Med Chem (1992) 35 : 734 -740
PubMed 1542100 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 6.54 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8569 1 7.85
CHEMBL8214 1 7.58
CHEMBL6616 1 7.52
CHEMBL292821 1 7.44
CHEMBL69700 1 7.30
CHEMBL6607 BROLAMFETAMINE 2.0 1 7.16
CHEMBL468880 1 7.08
CHEMBL317634 1 7.05
CHEMBL351858 1 7.01
CHEMBL60146 1 7.00
CHEMBL8224 1 7.00
CHEMBL162122 1 6.96
CHEMBL161905 1 6.89
CHEMBL8600 DOM 1 6.71
CHEMBL163985 1 6.66
CHEMBL166040 1 6.21
CHEMBL8642 1 5.92
CHEMBL61355 1 5.83
CHEMBL166041 1 5.83
CHEMBL162209 1 5.81
CHEMBL163814 1 5.71
CHEMBL6731 TENAMFETAMINE 2.0 1 5.68
CHEMBL8225 1 5.64
CHEMBL8389 1 5.57
CHEMBL282734 1 5.35
CHEMBL30336 1 5.24
CHEMBL273251 1 -
CHEMBL18762 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8569 Ki = 14.0 nM 7.85
CHEMBL8214 Ki = 26.0 nM 7.58
CHEMBL6616 Ki = 30.0 nM 7.52
CHEMBL292821 Ki = 36.0 nM 7.44
CHEMBL69700 Ki = 50.0 nM 7.30
CHEMBL6607 BROLAMFETAMINE Ki = 70.0 nM 7.16
CHEMBL468880 Ki = 84.0 nM 7.08
CHEMBL317634 Ki = 90.0 nM 7.05
CHEMBL351858 Ki = 98.0 nM 7.01
CHEMBL60146 Ki = 100.0 nM 7.00
CHEMBL8224 Ki = 101.0 nM 7.00
CHEMBL162122 Ki = 110.0 nM 6.96
CHEMBL161905 Ki = 130.0 nM 6.89
CHEMBL8600 DOM Ki = 193.0 nM 6.71
CHEMBL163985 Ki = 220.0 nM 6.66
CHEMBL166040 Ki = 610.0 nM 6.21
CHEMBL8642 Ki = 1217.0 nM 5.92
CHEMBL61355 Ki = 1485.0 nM 5.83
CHEMBL166041 Ki = 1480.0 nM 5.83
CHEMBL162209 Ki = 1560.0 nM 5.81
CHEMBL163814 Ki = 1935.0 nM 5.71
CHEMBL6731 TENAMFETAMINE Ki = 2100.0 nM 5.68
CHEMBL8225 Ki = 2300.0 nM 5.64
CHEMBL8389 Ki = 2666.0 nM 5.57
CHEMBL282734 Ki = 4475.0 nM 5.35
CHEMBL30336 Ki = 5710.0 nM 5.24
CHEMBL273251 Ki > 10000.0 nM -
CHEMBL18762 Ki > 10000.0 nM -