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

CHEMBL4146374

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

Binding
Displacement of [3H]-Ketanserin from human 5HT2AR expressed in CHO-K1 cell membranes after 1.5 hrs by microbeta counting method
5
Total Activities
5
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

Novel non-sulfonamide 5-HT6 receptor partial inverse agonist in a group of imidazo[4,5-b]pyridines with cognition enhancing properties.
Vanda D, Soural M, Canale V, Chaumont-Dubel S, Satała G, Kos T, Funk P, Fülöpová V, Lemrová B, Koczurkiewicz P, Pękala E, Bojarski AJ, Popik P, Marin P, Zajdel P.
Eur J Med Chem (2018) 144 : 716 -729
PubMed 29291439 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.55 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1083390 INTEPIRDINE 3.0 1 7.58
CHEMBL4175829 1 6.36
CHEMBL4164541 1 6.35
CHEMBL4169236 1 6.32
CHEMBL4161308 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1083390 INTEPIRDINE Ki = 26.0 nM 7.58
CHEMBL4175829 Ki = 441.0 nM 6.36
CHEMBL4164541 Ki = 449.0 nM 6.35
CHEMBL4169236 Ki = 475.0 nM 6.32
CHEMBL4161308 Ki = 694.0 nM 6.16