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Assay Detail

CHEMBL3783008

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

Binding
Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane after 2 hrs
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Dual Alleviation of Acute and Neuropathic Pain by Fused Opioid Agonist-Neurokinin 1 Antagonist Peptidomimetics.
Betti C, Starnowska J, Mika J, Dyniewicz J, Frankiewicz L, Novoa A, Bochynska M, Keresztes A, Kosson P, Makuch W, Van Duppen J, Chung NN, Vanden Broeck J, Lipkowski AW, Schiller PW, Janssens F, Ceusters M, Sommen F, Meert T, Przewlocka B, Tourwé D, Ballet S.
ACS Med Chem Lett (2015) 6 : 1209 -1214
PubMed 26713106 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 8.64 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3408519 1 10.10
CHEMBL3781680 1 9.73
CHEMBL1782141 1 9.38
CHEMBL2181202 1 9.24
CHEMBL3781519 1 8.93
CHEMBL3781336 1 8.74
CHEMBL3780686 1 8.51
CHEMBL3780776 1 8.00
CHEMBL3780818 1 7.70
CHEMBL3780408 1 7.40
CHEMBL3780820 1 7.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3408519 Ki = 0.08 nM 10.10
CHEMBL3781680 Ki = 0.187 nM 9.73
CHEMBL1782141 Ki = 0.42 nM 9.38
CHEMBL2181202 Ki = 0.58 nM 9.24
CHEMBL3781519 Ki = 1.18 nM 8.93
CHEMBL3781336 Ki = 1.82 nM 8.74
CHEMBL3780686 Ki = 3.07 nM 8.51
CHEMBL3780776 Ki = 9.91 nM 8.00
CHEMBL3780818 Ki = 20.2 nM 7.70
CHEMBL3780408 Ki = 39.8 nM 7.40
CHEMBL3780820 Ki = 54.0 nM 7.27