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Assay Detail

CHEMBL617534

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

Binding
Binding affinity against 5-hydroxytryptamine 2 receptor of rat frontal cortex using [3H]ketanserin radioligand
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Frontal cortex
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

A structure-affinity study of the binding of 4-substituted analogues of 1-(2,5-dimethoxyphenyl)-2-aminopropane at 5-HT2 serotonin receptors.
Seggel MR, Yousif MY, Lyon RA, Titeler M, Roth BL, Suba EA, Glennon RA.
J Med Chem (1990) 33 : 1032 -1036
PubMed 2308135 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 6.86 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL51 KETANSERIN 3.0 1 8.92
CHEMBL1204133 1 8.60
CHEMBL1204088 1 8.52
CHEMBL273770 1 8.15
CHEMBL1204089 1 8.15
CHEMBL1204134 1 8.00
CHEMBL6616 1 7.72
CHEMBL8317 1 7.72
CHEMBL6607 BROLAMFETAMINE 2.0 1 7.39
CHEMBL8214 1 7.24
CHEMBL8569 1 7.16
CHEMBL8237 1 7.12
CHEMBL8600 DOM 1 7.00
CHEMBL8224 1 7.00
CHEMBL8100 1 6.66
CHEMBL8301 1 6.52
CHEMBL267526 1 5.96
CHEMBL8389 1 5.90
CHEMBL8126 1 5.82
CHEMBL8225 1 5.66
CHEMBL1204090 1 5.62
CHEMBL273251 1 5.61
CHEMBL8642 1 5.28
CHEMBL416514 1 5.12
CHEMBL8028 1 4.58
CHEMBL1204087 1 -
CHEMBL8352 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL51 KETANSERIN Ki = 1.2 nM 8.92
CHEMBL1204133 Ki = 2.5 nM 8.60
CHEMBL1204088 Ki = 3.0 nM 8.52
CHEMBL273770 Ki = 7.0 nM 8.15
CHEMBL1204089 Ki = 7.0 nM 8.15
CHEMBL1204134 Ki = 10.0 nM 8.00
CHEMBL6616 Ki = 19.0 nM 7.72
CHEMBL8317 Ki = 19.0 nM 7.72
CHEMBL6607 BROLAMFETAMINE Ki = 41.0 nM 7.39
CHEMBL8214 Ki = 58.0 nM 7.24
CHEMBL8569 Ki = 69.0 nM 7.16
CHEMBL8237 Ki = 76.0 nM 7.12
CHEMBL8600 DOM Ki = 100.0 nM 7.00
CHEMBL8224 Ki = 100.0 nM 7.00
CHEMBL8100 Ki = 218.0 nM 6.66
CHEMBL8301 Ki = 300.0 nM 6.52
CHEMBL267526 Ki = 1100.0 nM 5.96
CHEMBL8389 Ki = 1250.0 nM 5.90
CHEMBL8126 Ki = 1530.0 nM 5.82
CHEMBL8225 Ki = 2200.0 nM 5.66
CHEMBL1204090 Ki = 2400.0 nM 5.62
CHEMBL273251 Ki = 2460.0 nM 5.61
CHEMBL8642 Ki = 5200.0 nM 5.28
CHEMBL416514 Ki = 7550.0 nM 5.12
CHEMBL8028 Ki = 26000.0 nM 4.58
CHEMBL1204087 Ki > 50000.0 nM -
CHEMBL8352 Ki > 50000.0 nM -