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Assay Detail

CHEMBL887388

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

Binding
Displacement of [3H]DAMGO from human mu opioid receptors expressed in CHO cell membrane
13
Total Activities
13
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

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

Publication

High-affinity carbamate analogues of morphinan at opioid receptors.
Peng X, Knapp BI, Bidlack JM, Neumeyer JL.
Bioorg Med Chem Lett (2007) 17 : 1508 -1511
PubMed 17276685 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 9.26 10.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49269 CYCLORPHAN 1 10.21
CHEMBL397035 1 9.96
CHEMBL242048 1 9.92
CHEMBL592 LEVORPHANOL 4.0 1 9.68
CHEMBL301160 BUTORPHAN 1 9.64
CHEMBL427862 1 9.54
CHEMBL263096 1 9.52
CHEMBL394624 1 9.15
CHEMBL242046 1 8.92
CHEMBL245049 1 8.85
CHEMBL242047 1 8.43
CHEMBL241823 1 8.32
CHEMBL241824 1 8.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49269 CYCLORPHAN Ki = 0.062 nM 10.21
CHEMBL397035 Ki = 0.11 nM 9.96
CHEMBL242048 Ki = 0.12 nM 9.92
CHEMBL592 LEVORPHANOL Ki = 0.21 nM 9.68
CHEMBL301160 BUTORPHAN Ki = 0.23 nM 9.64
CHEMBL427862 Ki = 0.29 nM 9.54
CHEMBL263096 Ki = 0.3 nM 9.52
CHEMBL394624 Ki = 0.7 nM 9.15
CHEMBL242046 Ki = 1.2 nM 8.92
CHEMBL245049 Ki = 1.4 nM 8.85
CHEMBL242047 Ki = 3.7 nM 8.43
CHEMBL241823 Ki = 4.8 nM 8.32
CHEMBL241824 Ki = 5.3 nM 8.28