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Assay Detail

CHEMBL5376115

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Binding
Agonist activity at MRGPRX4 83L (unknown origin) expressed in HEK293 cells co-expressing Gq assessed as change in intracellular calcium level by FLIPR assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of Potent Agonists for the Predominant Variant of the Orphan MAS-Related G Protein-Coupled Receptor X4 (MRGPRX4).
Marx D, Alnouri MW, Clemens S, Gedschold R, Riedel Y, Al Hamwi G, Pillaiyar T, Hockemeyer J, Namasivayam V, Müller CE.
J Med Chem (2023) 66 : 15674 -15698
PubMed 37967029 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 5.81 6.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5402204 1 6.83
CHEMBL5403433 1 6.24
CHEMBL783 NATEGLINIDE 4.0 1 5.33
CHEMBL412272 TAURODEOXYCHOLIC ACID 2.0 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5402204 EC50 = 149.0 nM 6.83
CHEMBL5403433 EC50 = 581.0 nM 6.24
CHEMBL783 NATEGLINIDE EC50 = 4720.0 nM 5.33
CHEMBL412272 TAURODEOXYCHOLIC ACID EC50 = 14100.0 nM 4.85