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Assay Detail

CHEMBL4124360

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

Binding
Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Pyrroloquinoline scaffold-based 5-HT6R ligands: Synthesis, quantum chemical and molecular dynamic studies, and influence of nitrogen atom position in the scaffold on affinity.
Grychowska K, Kurczab R, Śliwa P, Satała G, Dubiel K, Matłoka M, Moszczyński-Pętkowski R, Pieczykolan J, Bojarski AJ, Zajdel P.
Bioorg Med Chem (2018) 26 : 3588 -3595
PubMed 29853337 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.69 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1083390 INTEPIRDINE 3.0 1 8.85
CHEMBL4125735 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1083390 INTEPIRDINE Ki = 1.4 nM 8.85
CHEMBL4125735 Ki = 3.0 nM 8.52