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Assay Detail

CHEMBL754711

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

Binding
Binding affinity for opioid receptor type, human Opioid receptor mu 1 expressed in membrane homogenates of COS-1 or CHO cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type COS-1
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Mu-type opioid receptor (CHEMBL233)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist.
Halab L, Becker JA, Darula Z, Tourwé D, Kieffer BL, Simonin F, Lubell WD.
J Med Chem (2002) 45 : 5353 -5357
PubMed 12431062 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.61 7.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL358403 1 7.28
CHEMBL266609 1 7.12
CHEMBL140979 1 6.99
CHEMBL396460 NOCICEPTIN 1 6.57
CHEMBL2371034 1 6.43
CHEMBL355931 1 6.30
CHEMBL356210 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL358403 Ki = 53.0 nM 7.28
CHEMBL266609 Ki = 75.0 nM 7.12
CHEMBL140979 Ki = 102.0 nM 6.99
CHEMBL396460 NOCICEPTIN Ki = 270.0 nM 6.57
CHEMBL2371034 Ki = 368.0 nM 6.43
CHEMBL355931 Ki = 496.0 nM 6.30
CHEMBL356210 Ki = 2700.0 nM 5.57