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Assay Detail

CHEMBL4725977

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

Binding
Agonist activity at mouse FPR2 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric method
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Formyl peptide receptor 2 (CHEMBL4739842)
Type SINGLE PROTEIN
Organism Mus musculus

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 5 8.68 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4790836 1 9.20
CHEMBL4760897 1 8.85
CHEMBL4781596 1 8.82
CHEMBL4784510 BMS-986235 1.0 1 8.47
CHEMBL4762030 1 8.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4790836 EC50 = 0.63 nM 9.20
CHEMBL4760897 EC50 = 1.4 nM 8.85
CHEMBL4781596 EC50 = 1.5 nM 8.82
CHEMBL4784510 BMS-986235 EC50 = 3.4 nM 8.47
CHEMBL4762030 EC50 = 8.5 nM 8.07