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Assay Detail

CHEMBL1104717

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

Binding
Displacement of [3H]naloxone from human mu opioid receptor expressed in CHOK1 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane derivatives.
Geiger C, Zelenka C, Lehmkuhl K, Schepmann D, Englberger W, Wünsch B.
J Med Chem (2010) 53 : 4212 -4222
PubMed 20441176 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.21 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1094880 1 6.85
CHEMBL1096474 1 6.75
CHEMBL1095521 1 6.33
CHEMBL1094237 1 6.19
CHEMBL1096473 1 5.94
CHEMBL1096475 1 5.21
CHEMBL1095184 1 -
CHEMBL1094860 1 -
CHEMBL1094236 1 -
CHEMBL1095183 1 -
CHEMBL1096675 1 -
CHEMBL1095520 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1094880 Ki = 140.0 nM 6.85
CHEMBL1096474 Ki = 180.0 nM 6.75
CHEMBL1095521 Ki = 470.0 nM 6.33
CHEMBL1094237 Ki = 650.0 nM 6.19
CHEMBL1096473 Ki = 1150.0 nM 5.94
CHEMBL1096475 Ki = 6120.0 nM 5.21
CHEMBL1095184 Ki > 1000.0 nM -
CHEMBL1094860 Ki > 1000.0 nM -
CHEMBL1094236 Ki > 1000.0 nM -
CHEMBL1095183 Ki > 1000.0 nM -
CHEMBL1096675 Ki > 1000.0 nM -
CHEMBL1095520 Ki > 1000.0 nM -