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Assay Detail

CHEMBL4613002

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

Binding
Agonist activity at MRGPX2 (unknown origin)
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mas-related G-protein coupled receptor member X2 (CHEMBL5849)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Drug Discovery of <i>N</i>-((<i>R</i>)-3-(7-Methyl-1<i>H</i>-indazol-5-yl)-1-oxo-1-(((<i>S</i>)-1-oxo-3-(piperidin-4-yl)-1-(4-(pyridin-4-yl)piperazin-1-yl)propan-2-yl)amino)propan-2-yl)-2'-oxo-1',2'-dihydrospiro[piperidine-4,4'-pyrido[2,3-<i>d</i>][1,3]oxazine]-1-carboxamide (HTL22562): A Calcitonin Gene-Related Peptide Receptor Antagonist for Acute Treatment of Migraine.
Bucknell SJ, Ator MA, Brown AJH, Brown J, Cansfield AD, Cansfield JE, Christopher JA, Congreve M, Cseke G, Deflorian F, Jones CR, Mason JS, O'Brien MA, Ott GR, Pickworth M, Southall SM.
J Med Chem (2020) 63 : 7906 -7920
PubMed 32558564 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 6.05 6.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4635331 HTL-0022562 1.0 1 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4635331 HTL-0022562 EC50 = 900.0 nM 6.05