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Assay Detail

CHEMBL754508

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

Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Nociceptin receptor (CHEMBL2014)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel, potent ORL-1 receptor agonist peptides containing alpha-Helix-promoting conformational constraints.
Zhang C, Miller W, Valenzano KJ, Kyle DJ.
J Med Chem (2002) 45 : 5280 -5286
PubMed 12431054 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 8.80 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL414542 1 10.22
CHEMBL266191 1 10.10
CHEMBL408356 1 9.85
CHEMBL415845 1 9.70
CHEMBL264084 1 9.57
CHEMBL396460 NOCICEPTIN 1 9.35
CHEMBL410979 1 9.33
CHEMBL438537 1 9.14
CHEMBL415584 1 9.00
CHEMBL436732 1 8.28
CHEMBL405212 1 7.98
CHEMBL414543 1 7.28
CHEMBL427617 1 7.02
CHEMBL414541 1 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL414542 EC50 = 0.06 nM 10.22
CHEMBL266191 EC50 = 0.08 nM 10.10
CHEMBL408356 EC50 = 0.14 nM 9.85
CHEMBL415845 EC50 = 0.2 nM 9.70
CHEMBL264084 EC50 = 0.27 nM 9.57
CHEMBL396460 NOCICEPTIN EC50 = 0.45 nM 9.35
CHEMBL410979 EC50 = 0.47 nM 9.33
CHEMBL438537 EC50 = 0.73 nM 9.14
CHEMBL415584 EC50 = 1.0 nM 9.00
CHEMBL436732 EC50 = 5.3 nM 8.28
CHEMBL405212 EC50 = 10.5 nM 7.98
CHEMBL414543 EC50 = 52.0 nM 7.28
CHEMBL427617 EC50 = 96.0 nM 7.02
CHEMBL414541 EC50 = 407.0 nM 6.39