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Assay Detail

CHEMBL2330682

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

Binding
Displacement of [3H]diprenorphine from human KOR expressed in CHO cells after 1 hr by liquid scintillation counting analysis
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Kappa-type opioid receptor (CHEMBL237)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Opioid peptidomimetics: leads for the design of bioavailable mixed efficacy μ opioid receptor (MOR) agonist/δ opioid receptor (DOR) antagonist ligands.
Mosberg HI, Yeomans L, Harland AA, Bender AM, Sobczyk-Kojiro K, Anand JP, Clark MJ, Jutkiewicz EM, Traynor JR.
J Med Chem (2013) 56 : 2139 -2149
PubMed 23419026 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.24 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2322563 1 8.92
CHEMBL2322561 1 7.77
CHEMBL2322560 1 7.60
CHEMBL2322562 1 7.27
CHEMBL70 MORPHINE 4.0 1 7.21
CHEMBL2322568 1 7.17
CHEMBL2322567 1 6.96
CHEMBL2322566 1 6.89
CHEMBL2322564 1 6.66
CHEMBL2322565 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2322563 Ki = 1.2 nM 8.92
CHEMBL2322561 Ki = 17.0 nM 7.77
CHEMBL2322560 Ki = 25.0 nM 7.60
CHEMBL2322562 Ki = 54.0 nM 7.27
CHEMBL70 MORPHINE Ki = 60.9 nM 7.21
CHEMBL2322568 Ki = 68.0 nM 7.17
CHEMBL2322567 Ki = 110.0 nM 6.96
CHEMBL2322566 Ki = 130.0 nM 6.89
CHEMBL2322564 Ki = 220.0 nM 6.66
CHEMBL2322565 Ki = 1200.0 nM 5.92