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Assay Detail

CHEMBL5136529

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Functional
Agonist activity at human FPR1 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of Heteroaryl Urea Isosteres for Formyl Peptide Receptor 2 Agonists.
Wurtz NR, Johnson JA, Viet A, Shirude PS, Baligar V, Madduri S, Cheney DL, Park H, Lupisella JA, Hsu MY, Abousleiman M, Galella MA, Aulakh D, Dierks EA, Garcia RA, Ostrowski J, Kick EK, Wexler RR.
ACS Med Chem Lett (2022) 13 : 943 -948
PubMed 35707160 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 5.96 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4784510 BMS-986235 1.0 1 6.40
CHEMBL5191583 1 6.33
CHEMBL5190385 1 5.85
CHEMBL5187399 1 5.26
CHEMBL5186339 1 -
CHEMBL5208504 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4784510 BMS-986235 EC50 = 400.0 nM 6.40
CHEMBL5191583 EC50 = 470.0 nM 6.33
CHEMBL5190385 EC50 = 1400.0 nM 5.85
CHEMBL5187399 EC50 = 5500.0 nM 5.26
CHEMBL5186339 EC50 > 10000.0 nM -
CHEMBL5208504 EC50 > 10000.0 nM -