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Assay Detail

CHEMBL3766865

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

Binding
Displacement of [3H]DAMGO from rat cortical MOR by liquid scintillation counting method
11
Total Activities
11
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

Potent μ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[D-Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation.
Li Y, Cazares M, Wu J, Houghten RA, Toll L, Dooley C.
J Med Chem (2016) 59 : 1239 -1245
PubMed 26789491 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.83 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL316446 ENDOMORPHIN-1 1 9.15
CHEMBL3765059 1 9.00
CHEMBL3763920 1 8.71
CHEMBL3764556 1 8.70
CHEMBL3764157 1 8.04
CHEMBL3763985 1 8.04
CHEMBL3763495 1 7.85
CHEMBL3765741 1 7.76
CHEMBL3763905 1 6.94
CHEMBL3764234 1 6.00
CHEMBL3763452 1 5.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL316446 ENDOMORPHIN-1 Ki = 0.7 nM 9.15
CHEMBL3765059 Ki = 0.99 nM 9.00
CHEMBL3763920 Ki = 1.95 nM 8.71
CHEMBL3764556 Ki = 1.99 nM 8.70
CHEMBL3764157 Ki = 9.04 nM 8.04
CHEMBL3763985 Ki = 9.21 nM 8.04
CHEMBL3763495 Ki = 14.0 nM 7.85
CHEMBL3765741 Ki = 17.4 nM 7.76
CHEMBL3763905 Ki = 114.0 nM 6.94
CHEMBL3764234 Ki = 991.0 nM 6.00
CHEMBL3763452 Ki = 1129.0 nM 5.95