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Assay Detail

CHEMBL1015292

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Functional
Agonist activity at human MrgX1 receptor
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mas-related G-protein coupled receptor member X1 (CHEMBL5850)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of non-peptidergic MrgX1 and MrgX2 receptor agonists and exploration of an initial SAR using solid-phase synthesis.
Malik L, Kelly NM, Ma JN, Currier EA, Burstein ES, Olsson R.
Bioorg Med Chem Lett (2009) 19 : 1729 -1732
PubMed 19230660 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 6.34 7.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL502132 1 7.20
CHEMBL505263 1 6.70
CHEMBL466116 1 6.50
CHEMBL503202 1 6.50
CHEMBL501027 1 6.20
CHEMBL506128 1 6.10
CHEMBL474761 1 5.90
CHEMBL504032 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL502132 EC50 = 63.1 nM 7.20
CHEMBL505263 EC50 = 199.53 nM 6.70
CHEMBL466116 EC50 = 316.23 nM 6.50
CHEMBL503202 EC50 = 316.23 nM 6.50
CHEMBL501027 EC50 = 630.96 nM 6.20
CHEMBL506128 EC50 = 794.33 nM 6.10
CHEMBL474761 EC50 = 1258.93 nM 5.90
CHEMBL504032 EC50 = 2511.89 nM 5.60