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Assay Detail

CHEMBL4009142

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

Binding
Displacement of [3H]DAMGO from mu-type opioid receptor in guinea pig brain membranes after 120 mins by solid scintillation counting
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mu-type opioid receptor (CHEMBL4354)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective κ-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo.
Soeberdt M, Molenveld P, Storcken RP, Bouzanne des Mazery R, Sterk GJ, Autar R, Bolster MG, Wagner C, Aerts SN, van Holst FR, Wegert A, Tangherlini G, Frehland B, Schepmann D, Metze D, Lotts T, Knie U, Lin KY, Huang TY, Lai CC, Ständer S, Wünsch B, Abels C.
J Med Chem (2017) 60 : 2526 -2551
PubMed 28218838 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.78 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL80 NALOXONE 4.0 1 8.64
CHEMBL70 MORPHINE 4.0 1 8.28
CHEMBL4094571 1 7.68
CHEMBL3634516 1 7.37
CHEMBL4084350 1 7.04
CHEMBL4095192 1 6.74
CHEMBL4069231 1 6.66
CHEMBL4088788 1 6.51
CHEMBL4074031 1 6.47
CHEMBL4091184 1 6.44
CHEMBL4092100 1 6.29
CHEMBL4083401 1 6.26
CHEMBL4064380 1 6.21
CHEMBL4099849 1 6.08
CHEMBL4072972 1 5.91
CHEMBL4061582 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL80 NALOXONE Ki = 2.3 nM 8.64
CHEMBL70 MORPHINE Ki = 5.2 nM 8.28
CHEMBL4094571 Ki = 21.0 nM 7.68
CHEMBL3634516 Ki = 43.0 nM 7.37
CHEMBL4084350 Ki = 91.0 nM 7.04
CHEMBL4095192 Ki = 184.0 nM 6.74
CHEMBL4069231 Ki = 217.0 nM 6.66
CHEMBL4088788 Ki = 308.0 nM 6.51
CHEMBL4074031 Ki = 336.0 nM 6.47
CHEMBL4091184 Ki = 365.0 nM 6.44
CHEMBL4092100 Ki = 512.0 nM 6.29
CHEMBL4083401 Ki = 551.0 nM 6.26
CHEMBL4064380 Ki = 612.0 nM 6.21
CHEMBL4099849 Ki = 830.0 nM 6.08
CHEMBL4072972 Ki = 1230.0 nM 5.91
CHEMBL4061582 Ki = 1300.0 nM 5.89