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Assay Detail

CHEMBL5135849

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Binding
Binding affinity to 5HT6 receptor (unknown origin) assessed as inhibition constant
4
Total Activities
4
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

Discovery of Highly Potent Serotonin 5-HT<sub>2</sub> Receptor Agonists Inspired by Heteroyohimbine Natural Products.
Orr MJ, Cao AB, Wang CT, Gaisin A, Csakai A, Friswold AP, Meltzer HY, McCorvy JD, Scheidt KA.
ACS Med Chem Lett (2022) 13 : 648 -657
PubMed 35450369 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.08 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5207529 1 7.54
CHEMBL5170784 1 7.32
CHEMBL5204071 1 7.16
CHEMBL5182943 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5207529 Ki = 29.0 nM 7.54
CHEMBL5170784 Ki = 47.7 nM 7.32
CHEMBL5204071 Ki = 68.8 nM 7.16
CHEMBL5182943 Ki = 530.0 nM 6.28