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Assay Detail

CHEMBL1054181

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

Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Nociceptin receptor (CHEMBL4503)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discriminatory synergistic effect of Trp-substitutions in superagonist [(Arg/Lys)(14), (Arg/Lys)(15)]nociceptin on ORL1 receptor binding and activation.
Nishimura H, Li J, Isozaki K, Okada K, Matsushima A, Nose T, Costa T, Shimohigashi Y.
Bioorg Med Chem (2009) 17 : 5683 -5687
PubMed 19577933 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 9.43 9.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL505874 1 9.68
CHEMBL556388 1 9.64
CHEMBL559130 1 9.60
CHEMBL555757 1 9.52
CHEMBL558807 1 9.51
CHEMBL504587 1 9.39
CHEMBL510117 1 8.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL505874 IC50 = 0.21 nM 9.68
CHEMBL556388 IC50 = 0.23 nM 9.64
CHEMBL559130 IC50 = 0.25 nM 9.60
CHEMBL555757 IC50 = 0.3 nM 9.52
CHEMBL558807 IC50 = 0.31 nM 9.51
CHEMBL504587 IC50 = 0.41 nM 9.39
CHEMBL510117 IC50 = 2.1 nM 8.68