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Assay Detail

CHEMBL887069

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

Binding
Displacement of [3H]diprenorphine from human cloned delta 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

Delta-type opioid receptor (CHEMBL236)
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 7.96 9.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL247758 1 9.11
CHEMBL246572 1 9.00
CHEMBL246739 1 9.00
CHEMBL247760 1 8.92
CHEMBL246956 1 8.89
CHEMBL391580 1 8.74
CHEMBL13786 1 8.70
CHEMBL31421 1 8.49
CHEMBL246479 1 8.42
CHEMBL247368 1 8.00
CHEMBL247064 1 8.00
CHEMBL247759 1 7.72
CHEMBL247363 1 7.72
CHEMBL2372104 1 7.72
CHEMBL393867 1 7.38
CHEMBL246682 1 6.77
CHEMBL246740 1 6.44
CHEMBL392275 1 6.32
CHEMBL247163 1 5.96
CHEMBL395863 1 -
CHEMBL247562 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL247758 Ki = 0.78 nM 9.11
CHEMBL246572 Ki = 1.0 nM 9.00
CHEMBL246739 Ki = 1.0 nM 9.00
CHEMBL247760 Ki = 1.2 nM 8.92
CHEMBL246956 Ki = 1.3 nM 8.89
CHEMBL391580 Ki = 1.8 nM 8.74
CHEMBL13786 Ki = 2.0 nM 8.70
CHEMBL31421 Ki = 3.2 nM 8.49
CHEMBL246479 Ki = 3.8 nM 8.42
CHEMBL247368 Ki = 10.0 nM 8.00
CHEMBL247064 Ki = 10.0 nM 8.00
CHEMBL247759 Ki = 19.0 nM 7.72
CHEMBL247363 Ki = 19.0 nM 7.72
CHEMBL2372104 Ki = 19.0 nM 7.72
CHEMBL393867 Ki = 42.0 nM 7.38
CHEMBL246682 Ki = 170.0 nM 6.77
CHEMBL246740 Ki = 360.0 nM 6.44
CHEMBL392275 Ki = 475.0 nM 6.32
CHEMBL247163 Ki = 1100.0 nM 5.96
CHEMBL395863 Ki > 10000.0 nM -
CHEMBL247562 Ki > 10000.0 nM -