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Assay Detail

CHEMBL5167411

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

Binding
Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assay
61
Total Activities
61
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
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

Synthesis and Biological Characterization of a Series of 2-Sulfonamidebenzamides as Allosteric Modulators of MrgX1.
Sharma S, Peng Q, Vadukoot AK, Aretz CD, Jensen AA, Wallick AI, Dong X, Hopkins CR.
ACS Med Chem Lett (2022) 13 : 841 -847
PubMed 35586421 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 61 6.48 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5195160 1 7.89
CHEMBL5172913 1 7.85
CHEMBL5205606 1 7.51
CHEMBL5202767 1 7.27
CHEMBL5185447 1 7.26
CHEMBL5194692 1 7.16
CHEMBL5177145 1 7.10
CHEMBL5171656 1 7.01
CHEMBL5200001 1 6.99
CHEMBL5177388 1 6.91
CHEMBL5208855 1 6.76
CHEMBL5191110 1 6.69
CHEMBL5205025 1 6.66
CHEMBL5203677 1 6.54
CHEMBL5179980 1 6.44
CHEMBL5178316 1 6.43
CHEMBL5173653 1 6.39
CHEMBL5190176 1 6.36
CHEMBL5188039 1 6.30
CHEMBL5191409 1 6.30
CHEMBL5205161 1 6.07
CHEMBL5169615 1 6.04
CHEMBL5192837 1 5.98
CHEMBL5181857 1 5.96
CHEMBL5176049 1 5.87
CHEMBL5177134 1 5.85
CHEMBL5193744 1 5.55
CHEMBL5207586 1 5.50
CHEMBL5193017 1 5.04
CHEMBL5209542 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5195160 EC50 = 13.0 nM 7.89
CHEMBL5172913 EC50 = 14.0 nM 7.85
CHEMBL5205606 EC50 = 31.0 nM 7.51
CHEMBL5202767 EC50 = 54.0 nM 7.27
CHEMBL5185447 EC50 = 55.0 nM 7.26
CHEMBL5194692 EC50 = 69.0 nM 7.16
CHEMBL5177145 EC50 = 80.0 nM 7.10
CHEMBL5171656 EC50 = 98.0 nM 7.01
CHEMBL5200001 EC50 = 103.0 nM 6.99
CHEMBL5177388 EC50 = 124.0 nM 6.91
CHEMBL5208855 EC50 = 173.0 nM 6.76
CHEMBL5191110 EC50 = 206.0 nM 6.69
CHEMBL5205025 EC50 = 217.0 nM 6.66
CHEMBL5203677 EC50 = 285.0 nM 6.54
CHEMBL5179980 EC50 = 366.0 nM 6.44
CHEMBL5178316 EC50 = 369.0 nM 6.43
CHEMBL5173653 EC50 = 407.0 nM 6.39
CHEMBL5190176 EC50 = 435.0 nM 6.36
CHEMBL5188039 EC50 = 502.0 nM 6.30
CHEMBL5191409 EC50 = 506.0 nM 6.30
CHEMBL5205161 EC50 = 860.0 nM 6.07
CHEMBL5169615 EC50 = 915.0 nM 6.04
CHEMBL5192837 EC50 = 1040.0 nM 5.98
CHEMBL5181857 EC50 = 1090.0 nM 5.96
CHEMBL5176049 EC50 = 1360.0 nM 5.87
CHEMBL5177134 EC50 = 1400.0 nM 5.85
CHEMBL5193744 EC50 = 2830.0 nM 5.55
CHEMBL5207586 EC50 = 3140.0 nM 5.50
CHEMBL5193017 EC50 = 9010.0 nM 5.04
CHEMBL5209542 EC50 = 14200.0 nM 4.85
CHEMBL5209190 EC50 - -
CHEMBL5190795 EC50 - -
CHEMBL5197841 EC50 - -
CHEMBL5184689 EC50 - -
CHEMBL5181514 EC50 - -
CHEMBL5209208 EC50 - -
CHEMBL5172305 EC50 - -
CHEMBL5176103 EC50 - -
CHEMBL5171590 EC50 - -
CHEMBL5189843 EC50 - -
CHEMBL5173037 EC50 - -
CHEMBL5189972 EC50 - -
CHEMBL5199642 EC50 - -
CHEMBL5206207 EC50 - -
CHEMBL5186474 EC50 - -
CHEMBL5207415 EC50 - -
CHEMBL5202757 EC50 - -
CHEMBL5172368 EC50 - -
CHEMBL5207364 EC50 - -
CHEMBL5205222 EC50 - -