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Assay Detail

CHEMBL973302

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 cells
18
Total Activities
18
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

Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine.
Wentland MP, Sun X, Cohen DJ, Bidlack JM.
Bioorg Med Chem (2008) 16 : 5653 -5664
PubMed 18417347 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 7.60 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL377789 1 9.52
CHEMBL58646 1 9.51
CHEMBL469189 1 9.26
CHEMBL522375 1 9.26
CHEMBL493621 1 8.26
CHEMBL468857 1 8.16
CHEMBL494614 1 7.70
CHEMBL213880 1 7.57
CHEMBL463518 1 7.55
CHEMBL509054 1 7.50
CHEMBL511243 1 7.36
CHEMBL468182 1 7.06
CHEMBL495462 1 7.06
CHEMBL469188 1 6.77
CHEMBL512474 1 6.57
CHEMBL495461 1 6.20
CHEMBL502583 1 6.05
CHEMBL494613 1 5.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL377789 Ki = 0.3 nM 9.52
CHEMBL58646 Ki = 0.31 nM 9.51
CHEMBL469189 Ki = 0.55 nM 9.26
CHEMBL522375 Ki = 0.55 nM 9.26
CHEMBL493621 Ki = 5.5 nM 8.26
CHEMBL468857 Ki = 6.9 nM 8.16
CHEMBL494614 Ki = 20.0 nM 7.70
CHEMBL213880 Ki = 27.0 nM 7.57
CHEMBL463518 Ki = 28.0 nM 7.55
CHEMBL509054 Ki = 32.0 nM 7.50
CHEMBL511243 Ki = 44.0 nM 7.36
CHEMBL468182 Ki = 88.0 nM 7.06
CHEMBL495462 Ki = 88.0 nM 7.06
CHEMBL469188 Ki = 170.0 nM 6.77
CHEMBL512474 Ki = 270.0 nM 6.57
CHEMBL495461 Ki = 630.0 nM 6.20
CHEMBL502583 Ki = 890.0 nM 6.05
CHEMBL494613 Ki = 3800.0 nM 5.42