Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4725974

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

Binding
Agonist activity at human 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
ChEMBL ↗
44
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
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 44 8.90 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4776349 — — 1 10.30
CHEMBL4790836 — — 1 10.11
CHEMBL4743917 — — 1 10.07
CHEMBL4755590 — — 1 10.06
CHEMBL4744094 — — 2 10.04
CHEMBL4758920 — — 1 9.96
CHEMBL4784400 — — 1 9.96
CHEMBL4781596 — — 1 9.85
CHEMBL4744835 — — 1 9.82
CHEMBL4762030 — — 1 9.80
CHEMBL4761554 — — 1 9.72
CHEMBL4760897 — — 1 9.54
CHEMBL4778725 — — 1 9.49
CHEMBL4753713 — — 1 9.44
CHEMBL4784510 BMS-986235 1.0 1 9.39
CHEMBL4745044 — — 1 9.35
CHEMBL4749577 — — 1 9.12
CHEMBL4742149 — — 1 9.11
CHEMBL4740375 — — 2 9.05
CHEMBL4751168 — — 1 9.05
CHEMBL4793814 — — 1 9.04
CHEMBL4763824 — — 1 9.02
CHEMBL4781488 — — 1 8.85
CHEMBL4743084 — — 1 8.80
CHEMBL4790245 — — 1 8.72
CHEMBL4763673 — — 1 8.70
CHEMBL4793557 — — 1 8.51
CHEMBL4789579 — — 1 8.49
CHEMBL4796468 — — 1 8.44
CHEMBL4743133 — — 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4776349 — EC50 = 0.05 nM 10.30
CHEMBL4790836 — EC50 = 0.078 nM 10.11
CHEMBL4743917 — EC50 = 0.085 nM 10.07
CHEMBL4755590 — EC50 = 0.087 nM 10.06
CHEMBL4744094 — EC50 = 0.092 nM 10.04
CHEMBL4758920 — EC50 = 0.11 nM 9.96
CHEMBL4784400 — EC50 = 0.11 nM 9.96
CHEMBL4781596 — EC50 = 0.14 nM 9.85
CHEMBL4744835 — EC50 = 0.15 nM 9.82
CHEMBL4762030 — EC50 = 0.16 nM 9.80
CHEMBL4744094 — EC50 = 0.18 nM 9.74
CHEMBL4761554 — EC50 = 0.19 nM 9.72
CHEMBL4760897 — EC50 = 0.29 nM 9.54
CHEMBL4778725 — EC50 = 0.32 nM 9.49
CHEMBL4753713 — EC50 = 0.36 nM 9.44
CHEMBL4784510 BMS-986235 EC50 = 0.41 nM 9.39
CHEMBL4745044 — EC50 = 0.45 nM 9.35
CHEMBL4749577 — EC50 = 0.76 nM 9.12
CHEMBL4742149 — EC50 = 0.78 nM 9.11
CHEMBL4751168 — EC50 = 0.9 nM 9.05
CHEMBL4740375 — EC50 = 0.9 nM 9.05
CHEMBL4793814 — EC50 = 0.91 nM 9.04
CHEMBL4763824 — EC50 = 0.95 nM 9.02
CHEMBL4781488 — EC50 = 1.4 nM 8.85
CHEMBL4743084 — EC50 = 1.6 nM 8.80
CHEMBL4790245 — EC50 = 1.9 nM 8.72
CHEMBL4763673 — EC50 = 2.0 nM 8.70
CHEMBL4793557 — EC50 = 3.1 nM 8.51
CHEMBL4789579 — EC50 = 3.2 nM 8.49
CHEMBL4796468 — EC50 = 3.6 nM 8.44
CHEMBL4743133 — EC50 = 4.0 nM 8.40
CHEMBL4792002 — EC50 = 4.5 nM 8.35
CHEMBL4740375 — EC50 = 4.6 nM 8.34
CHEMBL4783963 — EC50 = 5.8 nM 8.24
CHEMBL4760555 — EC50 = 6.8 nM 8.17
CHEMBL4758129 — EC50 = 9.7 nM 8.01
CHEMBL4778312 — EC50 = 12.0 nM 7.92
CHEMBL4756320 — EC50 = 14.0 nM 7.85
CHEMBL4782531 — EC50 = 23.0 nM 7.64
CHEMBL4765025 — EC50 = 31.0 nM 7.51
CHEMBL4793603 — EC50 = 34.0 nM 7.47
CHEMBL4797598 — EC50 = 43.0 nM 7.37
CHEMBL1289260 — EC50 = 990.0 nM 6.00
CHEMBL4756217 — EC50 > 100.0 nM -