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

CHEMBL4736124

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

Binding
Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Subcellular Cell membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 6 (CHEMBL3371)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Imidazopyridine-Based 5-HT Receptor Neutral Antagonists: Impact of N-Benzyl and N-Phenylsulfonyl Fragments on Different Receptor Conformational States.
Vanda D,Canale V,Chaumont-Dubel S,Kurczab R,Satała G,Koczurkiewicz-Adamczyk P,Krawczyk M,Pietruś W,Blicharz K,Pękala E,Bojarski AJ,Popik P,Marin P,Soural M,Zajdel P
J Med Chem (2021) 64 : 1180 -1196
PubMed 33439019 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 8.26 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4756814 1 9.00
CHEMBL4760105 1 9.00
CHEMBL4760545 1 9.00
CHEMBL1083390 INTEPIRDINE 3.0 1 8.85
CHEMBL4777550 1 8.70
CHEMBL4756098 1 8.70
CHEMBL4759927 1 8.52
CHEMBL4743983 1 8.52
CHEMBL4742804 1 8.52
CHEMBL4756605 1 8.00
CHEMBL4799851 1 7.77
CHEMBL4783584 1 7.64
CHEMBL4746063 1 7.43
CHEMBL4758494 1 7.39
CHEMBL4784080 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4756814 Ki = 1.0 nM 9.00
CHEMBL4760105 Ki = 1.0 nM 9.00
CHEMBL4760545 Ki = 1.0 nM 9.00
CHEMBL1083390 INTEPIRDINE Ki = 1.4 nM 8.85
CHEMBL4777550 Ki = 2.0 nM 8.70
CHEMBL4756098 Ki = 2.0 nM 8.70
CHEMBL4759927 Ki = 3.0 nM 8.52
CHEMBL4743983 Ki = 3.0 nM 8.52
CHEMBL4742804 Ki = 3.0 nM 8.52
CHEMBL4756605 Ki = 10.0 nM 8.00
CHEMBL4799851 Ki = 17.0 nM 7.77
CHEMBL4783584 Ki = 23.0 nM 7.64
CHEMBL4746063 Ki = 37.0 nM 7.43
CHEMBL4758494 Ki = 41.0 nM 7.39
CHEMBL4784080 Ki = 119.0 nM 6.92