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Assay Detail

CHEMBL4725980

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Functional
Agonist activity at human FPR2 expressed in CHO cells assessed as reduction cAMP accumulation incubated for 1 hr by TR-FRET assay
1
Total Activities
1
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

N-formyl peptide receptor 2 (CHEMBL4227)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of BMS-986235/LAR-1219: A Potent Formyl Peptide Receptor 2 (FPR2) Selective Agonist for the Prevention of Heart Failure.
Asahina Y,Wurtz NR,Arakawa K,Carson N,Fujii K,Fukuchi K,Garcia R,Hsu MY,Ishiyama J,Ito B,Kick E,Lupisella J,Matsushima S,Ohata K,Ostrowski J,Saito Y,Tsuda K,Villarreal F,Yamada H,Yamaoka T,Wexler R,Gordon D,Kohno Y
J Med Chem (2020) 63 : 9003 -9019
PubMed 32407089 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 8.30 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4784510 BMS-986235 1.0 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4784510 BMS-986235 EC50 = 5.0 nM 8.30