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Assay Detail

CHEMBL5524115

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Functional
Agonist activity at human FPR1 expressed in HL-60 cells assessed as increase in calcium mobilization by FLIPR analysis
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HL-60
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

fMet-Leu-Phe receptor (CHEMBL3359)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The formyl peptide receptors FPR1 and FPR2 as targets for inflammatory disorders: recent advances in the development of small-molecule agonists.
Yi X, Tran E, Odiba JO, Qin CX, Ritchie RH, Baell JB.
Eur J Med Chem (2024) 265 : 115989 -115989
PubMed 38199163 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 5.87 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5568107 1 7.64
CHEMBL5563666 1 6.96
CHEMBL5561947 1 6.55
CHEMBL405908 1 6.52
CHEMBL329650 1 6.24
CHEMBL5568086 1 5.80
CHEMBL5561891 1 5.48
CHEMBL5562604 1 5.39
CHEMBL4162930 1 5.28
CHEMBL4173645 1 5.27
CHEMBL5562581 1 4.70
CHEMBL5563847 1 4.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5568107 EC50 = 23.0 nM 7.64
CHEMBL5563666 EC50 = 110.0 nM 6.96
CHEMBL5561947 EC50 = 280.0 nM 6.55
CHEMBL405908 EC50 = 300.0 nM 6.52
CHEMBL329650 EC50 = 570.0 nM 6.24
CHEMBL5568086 EC50 = 1600.0 nM 5.80
CHEMBL5561891 EC50 = 3300.0 nM 5.48
CHEMBL5562604 EC50 = 4100.0 nM 5.39
CHEMBL4162930 EC50 = 5200.0 nM 5.28
CHEMBL4173645 EC50 = 5400.0 nM 5.27
CHEMBL5562581 EC50 = 20000.0 nM 4.70
CHEMBL5563847 EC50 = 24000.0 nM 4.62