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Assay Detail

CHEMBL4352682

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

Functional
Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay
48
Total Activities
47
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

Substituted Pyridazin-3(2 H)-ones as Highly Potent and Biased Formyl Peptide Receptor Agonists.
Deora GS, Qin CX, Vecchio EA, Debono AJ, Priebbenow DL, Brady RM, Beveridge J, Teguh SC, Deo M, May LT, Krippner G, Ritchie RH, Baell JB.
J Med Chem (2019) 62 : 5242 -5248
PubMed 31038950 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 48 6.00 8.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4532583 1 8.19
CHEMBL379761 1 7.49
CHEMBL4536334 1 7.26
CHEMBL4447830 1 6.81
CHEMBL4447632 1 6.65
CHEMBL4454594 2 6.22
CHEMBL4476616 1 5.55
CHEMBL4551649 1 5.28
CHEMBL4549250 1 5.20
CHEMBL4551842 1 5.01
CHEMBL4448213 1 4.94
CHEMBL4442702 1 4.76
CHEMBL4588649 1 4.60
CHEMBL4436692 1 -
CHEMBL4581717 1 -
CHEMBL4536766 1 -
CHEMBL4459219 1 -
CHEMBL4571633 1 -
CHEMBL4556579 1 -
CHEMBL4581644 1 -
CHEMBL4446663 1 -
CHEMBL4440250 1 -
CHEMBL4517103 1 -
CHEMBL4560787 1 -
CHEMBL4569975 1 -
CHEMBL4453208 1 -
CHEMBL4440569 1 -
CHEMBL4436651 1 -
CHEMBL4452950 1 -
CHEMBL4568124 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4532583 EC50 = 6.457 nM 8.19
CHEMBL379761 EC50 = 32.36 nM 7.49
CHEMBL4536334 EC50 = 54.95 nM 7.26
CHEMBL4447830 EC50 = 154.88 nM 6.81
CHEMBL4447632 EC50 = 223.87 nM 6.65
CHEMBL4454594 EC50 = 603.0 nM 6.22
CHEMBL4454594 EC50 = 891.25 nM 6.05
CHEMBL4476616 EC50 = 2818.38 nM 5.55
CHEMBL4551649 EC50 = 5248.07 nM 5.28
CHEMBL4549250 EC50 = 6309.57 nM 5.20
CHEMBL4551842 EC50 = 9772.37 nM 5.01
CHEMBL4448213 EC50 = 11481.54 nM 4.94
CHEMBL4442702 EC50 = 17378.01 nM 4.76
CHEMBL4588649 EC50 = 25118.86 nM 4.60
CHEMBL4514037 EC50 > 100000.0 nM -
CHEMBL4547975 EC50 > 100000.0 nM -
CHEMBL4583846 EC50 > 100000.0 nM -
CHEMBL4539397 EC50 > 100000.0 nM -
CHEMBL4457243 EC50 > 100000.0 nM -
CHEMBL4472897 EC50 > 100000.0 nM -
CHEMBL4571633 EC50 > 100000.0 nM -
CHEMBL4452950 EC50 > 100000.0 nM -
CHEMBL556625 EC50 > 100000.0 nM -
CHEMBL551589 EC50 > 100000.0 nM -
CHEMBL4465768 EC50 > 100000.0 nM -
CHEMBL4448576 EC50 > 100000.0 nM -
CHEMBL4447184 EC50 > 100000.0 nM -
CHEMBL4440608 EC50 > 100000.0 nM -
CHEMBL4456812 EC50 > 100000.0 nM -
CHEMBL4473444 EC50 > 100000.0 nM -
CHEMBL4569975 EC50 > 100000.0 nM -
CHEMBL4436651 EC50 > 100000.0 nM -
CHEMBL4440250 EC50 > 100000.0 nM -
CHEMBL4543016 EC50 > 100000.0 nM -
CHEMBL4517103 EC50 > 100000.0 nM -
CHEMBL4446663 EC50 > 100000.0 nM -
CHEMBL4581644 EC50 > 100000.0 nM -
CHEMBL4556579 EC50 > 100000.0 nM -
CHEMBL4560787 EC50 > 100000.0 nM -
CHEMBL4568124 EC50 > 100000.0 nM -
CHEMBL4581435 EC50 > 100000.0 nM -
CHEMBL4440569 EC50 > 100000.0 nM -
CHEMBL4453208 EC50 > 100000.0 nM -
CHEMBL4549305 EC50 > 100000.0 nM -
CHEMBL4459219 EC50 > 100000.0 nM -
CHEMBL4536766 EC50 > 100000.0 nM -
CHEMBL4581717 EC50 > 100000.0 nM -
CHEMBL4436692 EC50 > 100000.0 nM -