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Assay Detail

CHEMBL5358336

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Functional
Agonist activity at NPFF2R (unknown origin) transfected in HEK293 cells co-expressing Galphaq15 assessed as increase in calcium mobilization by Fluo-4AM dye based assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuropeptide FF receptor 2 (CHEMBL5952)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

All-Hydrocarbon Stapled Peptide Multifunctional Agonists at Opioid and Neuropeptide FF Receptors: Highly Potent, Long-Lasting Brain Permeant Analgesics with Diminished Side Effects.
Zhang M, Xu B, Li N, Zhang Q, Chen D, Wu S, Yu B, Zhang X, Hu X, Zhang S, Jing Y, Yang Z, Jiang J, Fang Q.
J Med Chem (2023) 66 : 17138 -17154
PubMed 38095323 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 6.33 7.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5435869 1 7.48
CHEMBL5410237 1 7.28
CHEMBL429731 1 7.10
CHEMBL5428360 1 6.84
CHEMBL5401796 1 5.97
CHEMBL5430632 1 5.51
CHEMBL5427400 1 5.42
CHEMBL5406732 1 5.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5435869 EC50 = 33.1 nM 7.48
CHEMBL5410237 EC50 = 52.3 nM 7.28
CHEMBL429731 EC50 = 78.9 nM 7.10
CHEMBL5428360 EC50 = 144.3 nM 6.84
CHEMBL5401796 EC50 = 1076.0 nM 5.97
CHEMBL5430632 EC50 = 3110.0 nM 5.51
CHEMBL5427400 EC50 = 3756.0 nM 5.42
CHEMBL5406732 EC50 = 9766.0 nM 5.01