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Assay Detail

CHEMBL1677802

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

Binding
Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membrane by liquid scintillation counting
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Subcellular Membrane
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and pharmacological activities of 6-glycine substituted 14-phenylpropoxymorphinans, a novel class of opioids with high opioid receptor affinities and antinociceptive potencies.
Spetea M, Windisch P, Guo Y, Bileviciute-Ljungar I, Schütz J, Asim MF, Berzetei-Gurske IP, Riba P, Kiraly K, Fürst S, Al-Khrasani M, Schmidhammer H.
J Med Chem (2011) 54 : 980 -988
PubMed 21235243 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 8.96 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1672083 1 9.85
CHEMBL3216716 1 9.72
CHEMBL3216475 1 9.66
CHEMBL3216476 1 9.48
CHEMBL3216936 1 9.46
CHEMBL1672091 1 9.40
CHEMBL514774 1 9.32
CHEMBL1672087 1 9.04
CHEMBL1672086 1 9.00
CHEMBL1672090 1 8.96
CHEMBL1672085 1 8.11
CHEMBL1672084 1 7.81
CHEMBL70 MORPHINE 4.0 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1672083 Ki = 0.14 nM 9.85
CHEMBL3216716 Ki = 0.19 nM 9.72
CHEMBL3216475 Ki = 0.22 nM 9.66
CHEMBL3216476 Ki = 0.33 nM 9.48
CHEMBL3216936 Ki = 0.35 nM 9.46
CHEMBL1672091 Ki = 0.4 nM 9.40
CHEMBL514774 Ki = 0.48 nM 9.32
CHEMBL1672087 Ki = 0.92 nM 9.04
CHEMBL1672086 Ki = 1.01 nM 9.00
CHEMBL1672090 Ki = 1.11 nM 8.96
CHEMBL1672085 Ki = 7.86 nM 8.11
CHEMBL1672084 Ki = 15.4 nM 7.81
CHEMBL70 MORPHINE Ki = 217.0 nM 6.66