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Assay Detail

CHEMBL3411022

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

Binding
Displacement of [3H]DAMGO from rat brain MOR after 2 hrs
16
Total Activities
16
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

Synthesis and biological evaluation of compact, conformationally constrained bifunctional opioid agonist - neurokinin-1 antagonist peptidomimetics.
Guillemyn K, Kleczkowska P, Lesniak A, Dyniewicz J, Van der Poorten O, Van den Eynde I, Keresztes A, Varga E, Lai J, Porreca F, Chung NN, Lemieux C, Mika J, Rojewska E, Makuch W, Van Duppen J, Przewlocka B, Vanden Broeck J, Lipkowski AW, Schiller PW, Tourwé D, Ballet S.
Eur J Med Chem (2015) 92 : 64 -77
PubMed 25544687 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 9.67 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3408518 1 10.10
CHEMBL3408519 1 10.10
CHEMBL3408522 1 10.05
CHEMBL3408736 1 10.00
CHEMBL3408730 1 9.85
CHEMBL1782140 1 9.82
CHEMBL3408521 1 9.55
CHEMBL3408520 1 9.43
CHEMBL1782141 1 9.38
CHEMBL3408735 1 9.21
CHEMBL3408737 1 8.87
CHEMBL1782139 1 -
CHEMBL3408731 1 -
CHEMBL3408732 1 -
CHEMBL3408733 1 -
CHEMBL3408734 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3408518 Ki = 0.08 nM 10.10
CHEMBL3408519 Ki = 0.08 nM 10.10
CHEMBL3408522 Ki = 0.09 nM 10.05
CHEMBL3408736 Ki = 0.1 nM 10.00
CHEMBL3408730 Ki = 0.14 nM 9.85
CHEMBL1782140 Ki = 0.15 nM 9.82
CHEMBL3408521 Ki = 0.28 nM 9.55
CHEMBL3408520 Ki = 0.37 nM 9.43
CHEMBL1782141 Ki = 0.42 nM 9.38
CHEMBL3408735 Ki = 0.62 nM 9.21
CHEMBL3408737 Ki = 1.34 nM 8.87
CHEMBL1782139 Ki - -
CHEMBL3408731 Ki - -
CHEMBL3408732 Ki - -
CHEMBL3408733 Ki - -
CHEMBL3408734 Ki - -