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Assay Detail

CHEMBL5585743

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

Binding
Displacement of [3H]-LSD from human 5-HT6 receptor extracted from HEK293 cell membrane by microbeta plate reader analysis
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

5-HT<sub>6</sub> receptor neutral antagonists protect astrocytes: A lesson from 2-phenylpyrrole derivatives.
Drop M, Koczurkiewicz-Adamczyk P, Bento O, Pietruś W, Satała G, Blicharz-Futera K, Canale V, Grychowska K, Bantreil X, Pękala E, Kurczab R, Bojarski AJ, Chaumont-Dubel S, Marin P, Lamaty F, Zajdel P.
Eur J Med Chem (2024) 275 : 116615 -116615
PubMed 38936149 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 8.14 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5598162 1 9.00
CHEMBL5596350 1 9.00
CHEMBL5597256 1 9.00
CHEMBL1083390 INTEPIRDINE 3.0 1 8.89
CHEMBL5596691 1 8.70
CHEMBL5597727 1 8.70
CHEMBL5596980 1 8.40
CHEMBL5597355 1 8.40
CHEMBL5597650 1 8.40
CHEMBL5596555 1 8.10
CHEMBL5598097 1 7.90
CHEMBL5597198 1 7.60
CHEMBL5597699 1 7.57
CHEMBL5597062 1 7.38
CHEMBL5596507 1 7.35
CHEMBL5598057 1 7.16
CHEMBL5597928 1 6.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5598162 Ki = 1.0 nM 9.00
CHEMBL5596350 Ki = 1.0 nM 9.00
CHEMBL5597256 Ki = 1.0 nM 9.00
CHEMBL1083390 INTEPIRDINE Ki = 1.3 nM 8.89
CHEMBL5596691 Ki = 2.0 nM 8.70
CHEMBL5597727 Ki = 2.0 nM 8.70
CHEMBL5596980 Ki = 4.0 nM 8.40
CHEMBL5597355 Ki = 4.0 nM 8.40
CHEMBL5597650 Ki = 4.0 nM 8.40
CHEMBL5596555 Ki = 8.0 nM 8.10
CHEMBL5598097 Ki = 12.6 nM 7.90
CHEMBL5597198 Ki = 25.0 nM 7.60
CHEMBL5597699 Ki = 27.0 nM 7.57
CHEMBL5597062 Ki = 42.0 nM 7.38
CHEMBL5596507 Ki = 45.0 nM 7.35
CHEMBL5598057 Ki = 70.0 nM 7.16
CHEMBL5597928 Ki = 124.0 nM 6.91