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Assay Detail

CHEMBL3388385

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

Binding
Agonist activity at rat MrgX1 transfected in HEK293 cells by FLIPR assay
11
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mas-related G-protein coupled receptor member X1 (CHEMBL3341575)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Peptidomimetics of Arg-Phe-NH2 as small molecule agonists of Mas-related gene C (MrgC) receptors.
Hin N, Alt J, Zimmermann SC, Delahanty G, Ferraris DV, Rojas C, Li F, Liu Q, Dong X, Slusher BS, Tsukamoto T.
Bioorg Med Chem (2014) 22 : 5831 -5837
PubMed 25288495 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 5.47 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3343989 1 6.50
CHEMBL3343994 1 6.20
CHEMBL3343988 1 5.40
CHEMBL3343990 1 5.20
CHEMBL1672380 1 5.20
CHEMBL3343993 1 4.30
CHEMBL475965 1 -
CHEMBL3343987 1 -
CHEMBL3343991 1 -
CHEMBL3343992 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3343989 EC50 = 316.23 nM 6.50
CHEMBL3343994 EC50 = 630.96 nM 6.20
CHEMBL3343988 EC50 = 3981.07 nM 5.40
CHEMBL3343990 EC50 = 6309.57 nM 5.20
CHEMBL1672380 EC50 = 6309.57 nM 5.20
CHEMBL3343993 EC50 = 50118.72 nM 4.30
CHEMBL475965 EC50 > 1995.26 nM -
CHEMBL3343987 EC50 > 100000.0 nM -
CHEMBL3343991 EC50 > 100000.0 nM -
CHEMBL3343992 EC50 > 100000.0 nM -
CHEMBL3343992 EC50 > 100000.0 nM -