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Assay Detail

CHEMBL887070

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

Binding
Displacement of [3H]diprenorphine from human cloned kappa opioid receptor
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Further studies of tyrosine surrogates in opioid receptor peptide ligands.
Dolle RE, Michaut M, Martinez-Teipel B, Belanger S, Graczyk TM, DeHaven RN.
Bioorg Med Chem Lett (2007) 17 : 2656 -2660
PubMed 17350835 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 6.10 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL247368 1 6.68
CHEMBL246956 1 6.34
CHEMBL391580 1 5.99
CHEMBL246739 1 5.89
CHEMBL247758 1 5.62
CHEMBL246572 1 -
CHEMBL246479 1 -
CHEMBL247760 1 -
CHEMBL393867 1 -
CHEMBL246740 1 -
CHEMBL247759 1 -
CHEMBL392275 1 -
CHEMBL395863 1 -
CHEMBL13786 1 -
CHEMBL246682 1 -
CHEMBL247562 1 -
CHEMBL247163 1 -
CHEMBL247363 1 -
CHEMBL2372104 1 -
CHEMBL31421 1 -
CHEMBL247064 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL247368 Ki = 210.0 nM 6.68
CHEMBL246956 Ki = 460.0 nM 6.34
CHEMBL391580 Ki = 1030.0 nM 5.99
CHEMBL246739 Ki = 1300.0 nM 5.89
CHEMBL247758 Ki = 2400.0 nM 5.62
CHEMBL246572 Ki > 10000.0 nM -
CHEMBL246479 Ki > 10000.0 nM -
CHEMBL247760 Ki > 10000.0 nM -
CHEMBL393867 Ki > 10000.0 nM -
CHEMBL246740 Ki > 10000.0 nM -
CHEMBL247759 Ki > 10000.0 nM -
CHEMBL392275 Ki > 10000.0 nM -
CHEMBL395863 Ki > 10000.0 nM -
CHEMBL13786 Ki > 10000.0 nM -
CHEMBL246682 Ki > 10000.0 nM -
CHEMBL247562 Ki > 10000.0 nM -
CHEMBL247163 Ki > 10000.0 nM -
CHEMBL247363 Ki > 10000.0 nM -
CHEMBL2372104 Ki > 10000.0 nM -
CHEMBL31421 Ki > 10000.0 nM -
CHEMBL247064 Ki > 10000.0 nM -