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Assay Detail

CHEMBL896952

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

Binding
Displacement of [3H]DAMGO from human cloned mu opioid receptor
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Cinnamoyl derivatives of 7alpha-aminomethyl-6,14-endo-ethanotetrahydrothebaine and 7alpha-aminomethyl-6,14-endo-ethanotetrahydrooripavine and related opioid ligands.
Rennison D, Neal AP, Cami-Kobeci G, Aceto MD, Martinez-Bermejo F, Lewis JW, Husbands SM.
J Med Chem (2007) 50 : 5176 -5182
PubMed 17887741 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 9.05 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2113304 1 9.85
CHEMBL2113666 1 9.82
CHEMBL2113307 1 9.74
CHEMBL2113308 1 9.72
CHEMBL19019 NALTREXONE 4.0 1 9.70
CHEMBL2113313 1 9.66
CHEMBL2113306 1 9.64
CHEMBL2113303 1 9.60
CHEMBL2113305 1 9.60
CHEMBL2113311 1 9.41
CHEMBL2113314 1 9.32
CHEMBL2113296 1 9.20
CHEMBL2113312 1 9.17
CHEMBL2113295 1 9.13
CHEMBL2113299 1 9.06
CHEMBL70 MORPHINE 4.0 1 8.96
CHEMBL511142 BUPRENORPHINE 4.0 1 8.82
CHEMBL2113294 1 8.77
CHEMBL2113301 1 8.70
CHEMBL2113298 1 8.58
CHEMBL2113300 1 8.53
CHEMBL2113309 1 7.95
CHEMBL2113297 1 7.93
CHEMBL2113302 1 7.89
CHEMBL2113310 1 7.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2113304 Ki = 0.14 nM 9.85
CHEMBL2113666 Ki = 0.15 nM 9.82
CHEMBL2113307 Ki = 0.18 nM 9.74
CHEMBL2113308 Ki = 0.19 nM 9.72
CHEMBL19019 NALTREXONE Ki = 0.2 nM 9.70
CHEMBL2113313 Ki = 0.22 nM 9.66
CHEMBL2113306 Ki = 0.23 nM 9.64
CHEMBL2113303 Ki = 0.25 nM 9.60
CHEMBL2113305 Ki = 0.25 nM 9.60
CHEMBL2113311 Ki = 0.39 nM 9.41
CHEMBL2113314 Ki = 0.48 nM 9.32
CHEMBL2113296 Ki = 0.63 nM 9.20
CHEMBL2113312 Ki = 0.68 nM 9.17
CHEMBL2113295 Ki = 0.74 nM 9.13
CHEMBL2113299 Ki = 0.87 nM 9.06
CHEMBL70 MORPHINE Ki = 1.1 nM 8.96
CHEMBL511142 BUPRENORPHINE Ki = 1.5 nM 8.82
CHEMBL2113294 Ki = 1.69 nM 8.77
CHEMBL2113301 Ki = 1.98 nM 8.70
CHEMBL2113298 Ki = 2.61 nM 8.58
CHEMBL2113300 Ki = 2.96 nM 8.53
CHEMBL2113309 Ki = 11.3 nM 7.95
CHEMBL2113297 Ki = 11.8 nM 7.93
CHEMBL2113302 Ki = 12.8 nM 7.89
CHEMBL2113310 Ki = 34.2 nM 7.47