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Assay Detail

CHEMBL5376120

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

Binding
Agonist activity at MRGPRX4 83L (unknown origin) expressed in CHO cells assessed as induction of beta-arrestin recruitment measured after 90 mins by luminescence assay
25
Total Activities
25
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 25 5.11 6.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5402204 1 6.26
CHEMBL5408931 1 5.41
CHEMBL783 NATEGLINIDE 4.0 1 5.39
CHEMBL5420073 1 5.24
CHEMBL5408226 1 5.20
CHEMBL5403433 1 5.17
CHEMBL406393 DEOXYCHOLIC ACID 4.0 1 4.61
CHEMBL1551 URSODIOL 4.0 1 4.47
CHEMBL412272 TAURODEOXYCHOLIC ACID 2.0 1 4.25
CHEMBL1205720 1 -
CHEMBL5394109 1 -
CHEMBL5400164 1 -
CHEMBL5394574 1 -
CHEMBL5418196 1 -
CHEMBL5411533 1 -
CHEMBL5427570 1 -
CHEMBL5416729 1 -
CHEMBL5439076 1 -
CHEMBL5427296 1 -
CHEMBL5424935 1 -
CHEMBL5434279 1 -
CHEMBL5403197 1 -
CHEMBL5432461 1 -
CHEMBL5428142 1 -
CHEMBL5425100 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5402204 EC50 = 548.0 nM 6.26
CHEMBL5408931 EC50 = 3940.0 nM 5.41
CHEMBL783 NATEGLINIDE EC50 = 4090.0 nM 5.39
CHEMBL5420073 EC50 = 5710.0 nM 5.24
CHEMBL5408226 EC50 = 6280.0 nM 5.20
CHEMBL5403433 EC50 = 6700.0 nM 5.17
CHEMBL406393 DEOXYCHOLIC ACID EC50 = 24600.0 nM 4.61
CHEMBL1551 URSODIOL EC50 = 33800.0 nM 4.47
CHEMBL412272 TAURODEOXYCHOLIC ACID EC50 = 55700.0 nM 4.25
CHEMBL1205720 EC50 > 10000.0 nM -
CHEMBL5394109 EC50 > 10000.0 nM -
CHEMBL5400164 EC50 > 10000.0 nM -
CHEMBL5394574 EC50 > 10000.0 nM -
CHEMBL5418196 EC50 > 10000.0 nM -
CHEMBL5411533 EC50 > 10000.0 nM -
CHEMBL5427570 EC50 > 10000.0 nM -
CHEMBL5416729 EC50 > 10000.0 nM -
CHEMBL5439076 EC50 > 10000.0 nM -
CHEMBL5427296 EC50 > 10000.0 nM -
CHEMBL5424935 EC50 > 10000.0 nM -
CHEMBL5434279 EC50 > 10000.0 nM -
CHEMBL5403197 EC50 > 10000.0 nM -
CHEMBL5432461 EC50 > 10000.0 nM -
CHEMBL5428142 EC50 > 10000.0 nM -
CHEMBL5425100 EC50 > 10000.0 nM -