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Assay Detail

CHEMBL1100233

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

Binding
Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting
17
Total Activities
17
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 Autocuration

Target

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

Publication

Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors.
Fulton BS, Knapp BL, Bidlack JM, Neumeyer JL.
Bioorg Med Chem Lett (2010) 20 : 1507 -1509
PubMed 20144870 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 8.38 9.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1080925 1 9.68
CHEMBL301160 BUTORPHAN 1 9.64
CHEMBL1076579 1 9.62
CHEMBL1076572 1 9.02
CHEMBL1076573 1 8.92
CHEMBL1076578 1 8.62
CHEMBL1076576 1 8.49
CHEMBL1076577 1 8.32
CHEMBL1081608 1 8.19
CHEMBL1075629 1 8.15
CHEMBL1081084 1 8.14
CHEMBL1081250 1 8.13
CHEMBL1076575 1 7.92
CHEMBL1076574 1 7.77
CHEMBL348023 1 7.54
CHEMBL151872 1 7.18
CHEMBL1081093 1 7.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1080925 Ki = 0.21 nM 9.68
CHEMBL301160 BUTORPHAN Ki = 0.23 nM 9.64
CHEMBL1076579 Ki = 0.24 nM 9.62
CHEMBL1076572 Ki = 0.95 nM 9.02
CHEMBL1076573 Ki = 1.2 nM 8.92
CHEMBL1076578 Ki = 2.4 nM 8.62
CHEMBL1076576 Ki = 3.2 nM 8.49
CHEMBL1076577 Ki = 4.8 nM 8.32
CHEMBL1081608 Ki = 6.5 nM 8.19
CHEMBL1075629 Ki = 7.1 nM 8.15
CHEMBL1081084 Ki = 7.3 nM 8.14
CHEMBL1081250 Ki = 7.4 nM 8.13
CHEMBL1076575 Ki = 12.0 nM 7.92
CHEMBL1076574 Ki = 17.0 nM 7.77
CHEMBL348023 Ki = 29.0 nM 7.54
CHEMBL151872 Ki = 66.0 nM 7.18
CHEMBL1081093 Ki = 70.0 nM 7.16