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Assay Detail

CHEMBL5136528

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

Functional
Agonist activity at human FPR2 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assay
25
Total Activities
25
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 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 25 6.64 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4784510 BMS-986235 1.0 1 8.30
CHEMBL5191583 1 8.00
CHEMBL5190385 1 7.50
CHEMBL5201495 1 7.43
CHEMBL5185842 1 7.40
CHEMBL5181627 1 7.40
CHEMBL5197524 1 7.28
CHEMBL5169641 1 6.96
CHEMBL5204580 1 6.80
CHEMBL5187399 1 6.60
CHEMBL5201015 1 6.60
CHEMBL5208504 1 6.17
CHEMBL5203364 1 6.08
CHEMBL5186339 1 5.89
CHEMBL5197701 1 5.66
CHEMBL5204594 1 5.64
CHEMBL5194850 1 5.60
CHEMBL5195336 1 5.46
CHEMBL5203596 1 5.43
CHEMBL5180535 1 -
CHEMBL5207660 1 -
CHEMBL5195406 1 -
CHEMBL5208024 1 -
CHEMBL5174501 1 -
CHEMBL5192360 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4784510 BMS-986235 EC50 = 5.0 nM 8.30
CHEMBL5191583 EC50 = 10.0 nM 8.00
CHEMBL5190385 EC50 = 32.0 nM 7.50
CHEMBL5201495 EC50 = 37.0 nM 7.43
CHEMBL5185842 EC50 = 40.0 nM 7.40
CHEMBL5181627 EC50 = 40.0 nM 7.40
CHEMBL5197524 EC50 = 53.0 nM 7.28
CHEMBL5169641 EC50 = 110.0 nM 6.96
CHEMBL5204580 EC50 = 160.0 nM 6.80
CHEMBL5187399 EC50 = 250.0 nM 6.60
CHEMBL5201015 EC50 = 250.0 nM 6.60
CHEMBL5208504 EC50 = 680.0 nM 6.17
CHEMBL5203364 EC50 = 840.0 nM 6.08
CHEMBL5186339 EC50 = 1300.0 nM 5.89
CHEMBL5197701 EC50 = 2200.0 nM 5.66
CHEMBL5204594 EC50 = 2300.0 nM 5.64
CHEMBL5194850 EC50 = 2500.0 nM 5.60
CHEMBL5195336 EC50 = 3500.0 nM 5.46
CHEMBL5203596 EC50 = 3700.0 nM 5.43
CHEMBL5180535 EC50 > 10000.0 nM -
CHEMBL5207660 EC50 > 10000.0 nM -
CHEMBL5195406 EC50 > 10000.0 nM -
CHEMBL5208024 EC50 > 5000.0 nM -
CHEMBL5174501 EC50 > 10000.0 nM -
CHEMBL5192360 EC50 > 10000.0 nM -