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Assay Detail

CHEMBL830440

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

Binding
Inhibition of [125I]DOI binding to human 5-hydroxytryptamine 2A receptor expressed in CHO cells
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists.
Cole DC, Lennox WJ, Lombardi S, Ellingboe JW, Bernotas RC, Tawa GJ, Mazandarani H, Smith DL, Zhang G, Coupet J, Schechter LE.
J Med Chem (2005) 48 : 353 -356
PubMed 15658848 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 6.50 6.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL606556 1 6.57
CHEMBL606547 1 6.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL606556 Ki = 269.0 nM 6.57
CHEMBL606547 Ki = 367.0 nM 6.43