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Assay Detail

CHEMBL5042864

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

Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF2 receptor expressed in CHO cells by TopCount scintillation counting method
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Identification of an <i>N</i>-acylated-<sup>D</sup>Arg-Leu-NH<sub>2</sub> Dipeptide as a Highly Selective Neuropeptide FF1 Receptor Antagonist That Potently Prevents Opioid-Induced Hyperalgesia.
Quillet R, Schneider S, Utard V, Drieu la Rochelle A, Elhabazi K, Henningsen JB, Gizzi P, Schmitt M, Kugler V, Simonneaux V, Ilien B, Simonin F, Bihel F.
J Med Chem (2021) 64 : 7555 -7564
PubMed 34008968 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 6.56 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL429731 1 10.70
CHEMBL2165920 1 9.05
CHEMBL5093771 1 8.48
CHEMBL1672380 1 7.75
CHEMBL5082175 1 7.08
CHEMBL5084208 1 6.82
CHEMBL2208303 1 6.76
CHEMBL5090293 1 6.69
CHEMBL4776204 1 6.59
CHEMBL5071745 1 6.57
CHEMBL5087609 1 6.29
CHEMBL5075638 1 6.25
CHEMBL5088703 1 6.25
CHEMBL5074999 1 6.14
CHEMBL5085023 1 5.95
CHEMBL5093184 1 5.83
CHEMBL5091013 1 5.77
CHEMBL5082273 1 5.76
CHEMBL2208304 1 5.67
CHEMBL5085324 1 5.66
CHEMBL5076959 1 5.52
CHEMBL5088429 1 5.32
CHEMBL5091693 1 5.32
CHEMBL5082270 1 5.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL429731 Ki = 0.02 nM 10.70
CHEMBL2165920 Ki = 0.9 nM 9.05
CHEMBL5093771 Ki = 3.3 nM 8.48
CHEMBL1672380 Ki = 18.0 nM 7.75
CHEMBL5082175 Ki = 84.0 nM 7.08
CHEMBL5084208 Ki = 153.0 nM 6.82
CHEMBL2208303 Ki = 175.0 nM 6.76
CHEMBL5090293 Ki = 205.0 nM 6.69
CHEMBL4776204 Ki = 255.0 nM 6.59
CHEMBL5071745 Ki = 267.0 nM 6.57
CHEMBL5087609 Ki = 512.0 nM 6.29
CHEMBL5075638 Ki = 557.0 nM 6.25
CHEMBL5088703 Ki = 557.0 nM 6.25
CHEMBL5074999 Ki = 727.0 nM 6.14
CHEMBL5085023 Ki = 1113.0 nM 5.95
CHEMBL5093184 Ki = 1492.0 nM 5.83
CHEMBL5091013 Ki = 1685.0 nM 5.77
CHEMBL5082273 Ki = 1742.0 nM 5.76
CHEMBL2208304 Ki = 2150.0 nM 5.67
CHEMBL5085324 Ki = 2213.0 nM 5.66
CHEMBL5076959 Ki = 3045.0 nM 5.52
CHEMBL5088429 Ki = 4775.0 nM 5.32
CHEMBL5091693 Ki = 4838.0 nM 5.32
CHEMBL5082270 Ki = 6035.0 nM 5.22