Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1022744

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

Binding
Displacement of [3H]DAMGO from mu opioid receptor in Wistar rat brain
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

New endomorphin analogues containing alicyclic beta-amino acids: influence on bioactive conformation and pharmacological profile.
Keresztes A, Szucs M, Borics A, Kövér KE, Forró E, Fülöp F, Tömböly C, Péter A, Páhi A, Fábián G, Murányi M, Tóth G.
J Med Chem (2008) 51 : 4270 -4279
PubMed 18572932 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 7.32 9.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL316446 ENDOMORPHIN-1 1 9.13
CHEMBL333357 ENDOMORPHIN 2 1 8.89
CHEMBL450476 1 8.74
CHEMBL365583 1 8.62
CHEMBL363787 1 8.62
CHEMBL508249 1 8.44
CHEMBL506168 1 7.85
CHEMBL509619 1 7.80
CHEMBL447871 1 7.68
CHEMBL446990 1 7.07
CHEMBL455743 1 6.78
CHEMBL501894 1 6.56
CHEMBL467089 1 6.43
CHEMBL500623 1 6.13
CHEMBL472740 1 6.05
CHEMBL449748 1 5.99
CHEMBL372682 1 5.70
CHEMBL192506 1 5.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL316446 ENDOMORPHIN-1 Ki = 0.74 nM 9.13
CHEMBL333357 ENDOMORPHIN 2 Ki = 1.3 nM 8.89
CHEMBL450476 Ki = 1.8 nM 8.74
CHEMBL365583 Ki = 2.4 nM 8.62
CHEMBL363787 Ki = 2.4 nM 8.62
CHEMBL508249 Ki = 3.6 nM 8.44
CHEMBL506168 Ki = 14.0 nM 7.85
CHEMBL509619 Ki = 16.0 nM 7.80
CHEMBL447871 Ki = 21.0 nM 7.68
CHEMBL446990 Ki = 86.0 nM 7.07
CHEMBL455743 Ki = 166.0 nM 6.78
CHEMBL501894 Ki = 275.0 nM 6.56
CHEMBL467089 Ki = 374.0 nM 6.43
CHEMBL500623 Ki = 741.0 nM 6.13
CHEMBL472740 Ki = 883.0 nM 6.05
CHEMBL449748 Ki = 1033.0 nM 5.99
CHEMBL372682 Ki = 1984.0 nM 5.70
CHEMBL192506 Ki = 4435.0 nM 5.35