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Assay Detail

CHEMBL4135884

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Functional
Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel ureidopropanamide based N-formyl peptide receptor 2 (FPR2) agonists with potential application for central nervous system disorders characterized by neuroinflammation.
Stama ML, Ślusarczyk J, Lacivita E, Kirpotina LN, Schepetkin IA, Chamera K, Riganti C, Perrone R, Quinn MT, Basta-Kaim A, Leopoldo M.
Eur J Med Chem (2017) 141 : 703 -720
PubMed 29102463 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 5.57 6.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4159569 1 6.35
CHEMBL4170201 1 6.20
CHEMBL4164673 1 6.07
CHEMBL4168567 1 6.02
CHEMBL4172556 1 5.82
CHEMBL4176353 1 5.62
CHEMBL4172968 1 5.55
CHEMBL4162303 1 5.33
CHEMBL4162930 1 5.28
CHEMBL4173645 1 5.27
CHEMBL4169807 1 5.23
CHEMBL4166385 1 4.99
CHEMBL4166447 1 4.73
CHEMBL4165740 1 -
CHEMBL4169174 1 -
CHEMBL4161249 1 -
CHEMBL4170646 1 -
CHEMBL4162715 1 -
CHEMBL4177002 1 -
CHEMBL4161887 1 -
CHEMBL4174852 1 -
CHEMBL4161946 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4159569 EC50 = 450.0 nM 6.35
CHEMBL4170201 EC50 = 630.0 nM 6.20
CHEMBL4164673 EC50 = 850.0 nM 6.07
CHEMBL4168567 EC50 = 950.0 nM 6.02
CHEMBL4172556 EC50 = 1500.0 nM 5.82
CHEMBL4176353 EC50 = 2400.0 nM 5.62
CHEMBL4172968 EC50 = 2800.0 nM 5.55
CHEMBL4162303 EC50 = 4700.0 nM 5.33
CHEMBL4162930 EC50 = 5200.0 nM 5.28
CHEMBL4173645 EC50 = 5400.0 nM 5.27
CHEMBL4169807 EC50 = 5900.0 nM 5.23
CHEMBL4166385 EC50 = 10300.0 nM 4.99
CHEMBL4166447 EC50 = 18800.0 nM 4.73
CHEMBL4165740 EC50 - -
CHEMBL4169174 EC50 - -
CHEMBL4161249 EC50 - -
CHEMBL4170646 EC50 - -
CHEMBL4162715 EC50 - -
CHEMBL4177002 EC50 - -
CHEMBL4161887 EC50 - -
CHEMBL4174852 EC50 - -
CHEMBL4161946 EC50 - -