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Assay Detail

CHEMBL750840

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

Binding
Inhibition of [3H]- bremazocine to opioid receptor kappa of guinea pig cerebral membranes was determined
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Kappa-type opioid receptor (CHEMBL3952)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Effect of modification of the basic residues of dynorphin A-(1-13) amide on kappa opioid receptor selectivity and opioid activity.
Snyder KR, Story SC, Heidt ME, Murray TF, DeLander GE, Aldrich JV.
J Med Chem (1992) 35 : 4330 -4333
PubMed 1360025 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 10.37 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL266717 1 10.70
CHEMBL266515 1 10.68
CHEMBL415330 1 10.64
CHEMBL438741 1 10.62
CHEMBL440446 1 10.28
CHEMBL263583 1 9.85
CHEMBL263597 1 9.82
CHEMBL415617 1 -
CHEMBL440987 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL266717 Ki = 0.02 nM 10.70
CHEMBL266515 Ki = 0.021 nM 10.68
CHEMBL415330 Ki = 0.023 nM 10.64
CHEMBL438741 Ki = 0.024 nM 10.62
CHEMBL440446 Ki = 0.053 nM 10.28
CHEMBL263583 Ki = 0.14 nM 9.85
CHEMBL263597 Ki = 0.15 nM 9.82
CHEMBL415617 Ki = 0.0067 nM -
CHEMBL440987 Ki = 0.0042 nM -