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Assay Detail

CHEMBL4146403

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

Binding
Binding affinity to 5HT6R (unknown origin)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 6 (CHEMBL3371)
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 7 9.06 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4170220 1 9.70
CHEMBL1083390 INTEPIRDINE 3.0 1 9.55
CHEMBL4169827 1 9.52
CHEMBL3286580 IDALOPIRDINE 3.0 1 9.08
CHEMBL370779 1 9.00
CHEMBL4161904 1 8.30
CHEMBL4177024 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4170220 Ki = 0.2 nM 9.70
CHEMBL1083390 INTEPIRDINE Ki = 0.28 nM 9.55
CHEMBL4169827 Ki = 0.3 nM 9.52
CHEMBL3286580 IDALOPIRDINE Ki = 0.83 nM 9.08
CHEMBL370779 Ki = 1.0 nM 9.00
CHEMBL4161904 Ki = 5.0 nM 8.30
CHEMBL4177024 Ki = 5.0 nM 8.30