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Assay Detail

CHEMBL759235

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

Binding
Inhibition of [3H]DAGO binding to rat brain membrane Opioid receptor mu 1
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Mu-type opioid receptor (CHEMBL270)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Development of conformationally constrained linear peptides exhibiting a high affinity and pronounced selectivity for delta opioid receptors.
Gacel G, Daugé V, Breuzé P, Delay-Goyet P, Roques BP.
J Med Chem (1988) 31 : 1891 -1897
PubMed 2845081 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.74 7.63

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55734 1 7.63
CHEMBL13786 1 7.56
CHEMBL124283 1 7.51
CHEMBL57776 1 7.38
CHEMBL55498 1 7.19
CHEMBL299029 1 6.73
CHEMBL298972 1 6.43
CHEMBL56933 1 6.32
CHEMBL31421 1 6.06
CHEMBL301702 1 6.00
CHEMBL56394 1 5.35
CHEMBL299497 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55734 Ki = 23.3 nM 7.63
CHEMBL13786 Ki = 27.5 nM 7.56
CHEMBL124283 Ki = 31.0 nM 7.51
CHEMBL57776 Ki = 42.1 nM 7.38
CHEMBL55498 Ki = 64.6 nM 7.19
CHEMBL299029 Ki = 185.0 nM 6.73
CHEMBL298972 Ki = 374.0 nM 6.43
CHEMBL56933 Ki = 475.0 nM 6.32
CHEMBL31421 Ki = 873.0 nM 6.06
CHEMBL301702 Ki = 993.0 nM 6.00
CHEMBL56394 Ki = 4500.0 nM 5.35
CHEMBL299497 Ki > 100000.0 nM -