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Assay Detail

CHEMBL5035397

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

Functional
Agonist activity at NPFF2R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
18
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Development of Multifunctional and Orally Active Cyclic Peptide Agonists of Opioid/Neuropeptide FF Receptors that Produce Potent, Long-Lasting, and Peripherally Restricted Antinociception with Diminished Side Effects.
Zhang M, Xu B, Li N, Zhang R, Zhang Q, Shi X, Xu K, Xiao J, Chen D, Niu J, Shi Y, Fang Q.
J Med Chem (2021) 64 : 13394 -13409
PubMed 34465090 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 6.87 7.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL429731 2 7.37
CHEMBL5085455 2 7.30
CHEMBL5085013 2 7.09
CHEMBL5086601 2 6.95
CHEMBL5094675 2 6.88
CHEMBL5086463 2 6.72
CHEMBL5091560 2 6.58
CHEMBL5090298 2 6.52
CHEMBL5082892 2 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL429731 EC50 = 42.66 nM 7.37
CHEMBL429731 EC50 = 42.4 nM 7.37
CHEMBL5085455 EC50 = 49.8 nM 7.30
CHEMBL5085455 EC50 = 50.12 nM 7.30
CHEMBL5085013 EC50 = 81.28 nM 7.09
CHEMBL5085013 EC50 = 81.5 nM 7.09
CHEMBL5086601 EC50 = 112.0 nM 6.95
CHEMBL5086601 EC50 = 112.2 nM 6.95
CHEMBL5094675 EC50 = 133.0 nM 6.88
CHEMBL5094675 EC50 = 131.83 nM 6.88
CHEMBL5086463 EC50 = 190.55 nM 6.72
CHEMBL5086463 EC50 = 190.0 nM 6.72
CHEMBL5091560 EC50 = 263.03 nM 6.58
CHEMBL5091560 EC50 = 265.0 nM 6.58
CHEMBL5090298 EC50 = 303.0 nM 6.52
CHEMBL5090298 EC50 = 309.03 nM 6.51
CHEMBL5082892 EC50 = 349.0 nM 6.46
CHEMBL5082892 EC50 = 354.81 nM 6.45