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

CHEMBL4366765

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

Binding
Displacement of [3H]-Ketanserin from human 5-HT2A expressed in CHO-K1 cells incubated for 1.5 hrs by radioligand binding assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and computer-aided SAR studies for derivatives of phenoxyalkyl-1,3,5-triazine as the new potent ligands for serotonin receptors 5-HT<sub>6</sub>.
Ali W, Więcek M, Łażewska D, Kurczab R, Jastrzębska-Więsek M, Satała G, Kucwaj-Brysz K, Lubelska A, Głuch-Lutwin M, Mordyl B, Siwek A, Nasim MJ, Partyka A, Sudoł S, Latacz G, Wesołowska A, Kieć-Kononowicz K, Handzlik J.
Eur J Med Chem (2019) 178 : 740 -751
PubMed 31229876 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 5.99 6.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4527124 1 6.71
CHEMBL4557247 1 6.71
CHEMBL4462404 1 6.42
CHEMBL4515075 1 6.39
CHEMBL4580959 1 6.39
CHEMBL4520796 1 6.37
CHEMBL4522568 1 6.23
CHEMBL4447416 1 5.74
CHEMBL4532712 1 5.64
CHEMBL4465929 1 5.58
CHEMBL4441655 1 4.94
CHEMBL4570584 1 4.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4527124 Ki = 197.0 nM 6.71
CHEMBL4557247 Ki = 197.0 nM 6.71
CHEMBL4462404 Ki = 376.0 nM 6.42
CHEMBL4515075 Ki = 407.0 nM 6.39
CHEMBL4580959 Ki = 406.0 nM 6.39
CHEMBL4520796 Ki = 430.0 nM 6.37
CHEMBL4522568 Ki = 590.0 nM 6.23
CHEMBL4447416 Ki = 1830.0 nM 5.74
CHEMBL4532712 Ki = 2274.0 nM 5.64
CHEMBL4465929 Ki = 2628.0 nM 5.58
CHEMBL4441655 Ki = 11590.0 nM 4.94
CHEMBL4570584 Ki = 17170.0 nM 4.76