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Assay Detail

CHEMBL621544

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

Binding
Binding affinity towards 5-hydroxytryptamine 2A receptor sites by using [3H]ketanserin as radioligand
15
Total Activities
15
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 2A (CHEMBL322)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Ring substituted analogues of 5-aminomethyl-10,11-dihydro-dibenzo[a,d]cycloheptene (AMDH): potential modes of binding to the 5-HT(2A) receptor.
Peddi S, Roth BL, Glennon RA, Westkaemper RB.
Bioorg Med Chem Lett (2003) 13 : 2565 -2568
PubMed 12852967 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.35 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85882 1 8.89
CHEMBL268890 1 8.60
CHEMBL83082 1 8.49
CHEMBL86760 1 8.15
CHEMBL83081 1 8.12
CHEMBL8334 1 8.00
CHEMBL47482 1 7.70
CHEMBL87648 1 7.43
CHEMBL6607 BROLAMFETAMINE 2.0 1 7.39
CHEMBL85718 1 7.09
CHEMBL44819 1 6.96
CHEMBL83028 1 6.20
CHEMBL313694 1 6.10
CHEMBL8389 1 5.92
CHEMBL8642 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85882 Ki = 1.3 nM 8.89
CHEMBL268890 Ki = 2.5 nM 8.60
CHEMBL83082 Ki = 3.2 nM 8.49
CHEMBL86760 Ki = 7.0 nM 8.15
CHEMBL83081 Ki = 7.5 nM 8.12
CHEMBL8334 Ki = 10.0 nM 8.00
CHEMBL47482 Ki = 20.0 nM 7.70
CHEMBL87648 Ki = 37.0 nM 7.43
CHEMBL6607 BROLAMFETAMINE Ki = 41.0 nM 7.39
CHEMBL85718 Ki = 81.0 nM 7.09
CHEMBL44819 Ki = 110.0 nM 6.96
CHEMBL83028 Ki = 630.0 nM 6.20
CHEMBL313694 Ki = 800.0 nM 6.10
CHEMBL8389 Ki = 1200.0 nM 5.92
CHEMBL8642 Ki = 5200.0 nM 5.28