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Assay Detail

CHEMBL829148

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Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
8
Total Activities
8
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 Expert

Target

Nociceptin receptor (CHEMBL2014)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N- and C-terminal modifications of nociceptin/orphanin FQ generate highly potent NOP receptor ligands.
Guerrini R, Caló G, Lambert DG, Carrá G, Arduin M, Barnes TA, McDonald J, Rizzi D, Trapella C, Marzola E, Rowbotham DJ, Regoli D, Salvadori S.
J Med Chem (2005) 48 : 1421 -1427
PubMed 15743186 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 9.32 10.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL414782 1 10.12
CHEMBL410653 1 9.85
CHEMBL442297 1 9.68
CHEMBL264846 1 9.51
CHEMBL263588 1 9.09
CHEMBL262544 1 9.03
CHEMBL396460 NOCICEPTIN 1 8.98
CHEMBL414767 1 8.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL414782 EC50 = 0.07586 nM 10.12
CHEMBL410653 EC50 = 0.1413 nM 9.85
CHEMBL442297 EC50 = 0.2089 nM 9.68
CHEMBL264846 EC50 = 0.309 nM 9.51
CHEMBL263588 EC50 = 0.8128 nM 9.09
CHEMBL262544 EC50 = 0.9333 nM 9.03
CHEMBL396460 NOCICEPTIN EC50 = 1.047 nM 8.98
CHEMBL414767 EC50 = 5.248 nM 8.28