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Assay Detail

CHEMBL754586

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
Ki 14 9.40 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415845 1 10.70
CHEMBL266191 1 10.30
CHEMBL414542 1 10.30
CHEMBL438537 1 10.22
CHEMBL408356 1 10.10
CHEMBL264084 1 10.00
CHEMBL410979 1 9.82
CHEMBL396460 NOCICEPTIN 1 9.52
CHEMBL415584 1 9.32
CHEMBL436732 1 8.96
CHEMBL405212 1 8.66
CHEMBL414543 1 8.17
CHEMBL427617 1 7.82
CHEMBL414541 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415845 Ki = 0.02 nM 10.70
CHEMBL266191 Ki = 0.05 nM 10.30
CHEMBL414542 Ki = 0.05 nM 10.30
CHEMBL438537 Ki = 0.06 nM 10.22
CHEMBL408356 Ki = 0.08 nM 10.10
CHEMBL264084 Ki = 0.1 nM 10.00
CHEMBL410979 Ki = 0.15 nM 9.82
CHEMBL396460 NOCICEPTIN Ki = 0.3 nM 9.52
CHEMBL415584 Ki = 0.48 nM 9.32
CHEMBL436732 Ki = 1.1 nM 8.96
CHEMBL405212 Ki = 2.2 nM 8.66
CHEMBL414543 Ki = 6.7 nM 8.17
CHEMBL427617 Ki = 15.0 nM 7.82
CHEMBL414541 Ki = 20.0 nM 7.70