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Assay Detail

CHEMBL901091

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

Binding
Displacement of [3H]bremazocine from cloned human delta opioid receptor expressed in CHO cells
28
Total Activities
28
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 Intermediate

Target

Delta-type opioid receptor (CHEMBL236)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.
Takeuchi K, Holloway WG, Mitch CH, Quimby SJ, McKinzie JH, Suter TM, Statnick MA, Surface PL, Emmerson PJ, Thomas EM, Siegel MG.
Bioorg Med Chem Lett (2007) 17 : 6841 -6846
PubMed 17980586 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 6.50 8.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL238361 1 8.94
CHEMBL300662 1 8.32
CHEMBL19019 NALTREXONE 4.0 1 7.79
CHEMBL237066 1 7.15
CHEMBL396636 1 6.97
CHEMBL237295 1 6.84
CHEMBL237716 1 6.79
CHEMBL237073 1 6.77
CHEMBL397148 1 6.75
CHEMBL237506 1 6.73
CHEMBL237718 1 6.63
CHEMBL237934 1 6.62
CHEMBL439038 1 6.41
CHEMBL396637 1 6.39
CHEMBL238157 1 6.33
CHEMBL237505 1 6.30
CHEMBL237294 1 5.86
CHEMBL238363 1 5.72
CHEMBL237071 1 5.67
CHEMBL235154 1 5.64
CHEMBL235155 1 5.63
CHEMBL398089 1 5.61
CHEMBL238364 1 5.59
CHEMBL237293 1 5.57
CHEMBL238156 1 5.41
CHEMBL237072 1 -
CHEMBL238362 1 -
CHEMBL398090 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL238361 Ki = 1.16 nM 8.94
CHEMBL300662 Ki = 4.82 nM 8.32
CHEMBL19019 NALTREXONE Ki = 16.31 nM 7.79
CHEMBL237066 Ki = 70.21 nM 7.15
CHEMBL396636 Ki = 107.88 nM 6.97
CHEMBL237295 Ki = 144.07 nM 6.84
CHEMBL237716 Ki = 163.22 nM 6.79
CHEMBL237073 Ki = 169.39 nM 6.77
CHEMBL397148 Ki = 179.6 nM 6.75
CHEMBL237506 Ki = 187.0 nM 6.73
CHEMBL237718 Ki = 232.46 nM 6.63
CHEMBL237934 Ki = 239.77 nM 6.62
CHEMBL439038 Ki = 388.15 nM 6.41
CHEMBL396637 Ki = 409.29 nM 6.39
CHEMBL238157 Ki = 466.27 nM 6.33
CHEMBL237505 Ki = 503.7 nM 6.30
CHEMBL237294 Ki = 1377.0 nM 5.86
CHEMBL238363 Ki = 1909.0 nM 5.72
CHEMBL237071 Ki = 2139.0 nM 5.67
CHEMBL235154 Ki = 2274.0 nM 5.64
CHEMBL235155 Ki = 2351.0 nM 5.63
CHEMBL398089 Ki = 2448.94 nM 5.61
CHEMBL238364 Ki = 2576.0 nM 5.59
CHEMBL237293 Ki = 2708.0 nM 5.57
CHEMBL238156 Ki = 3888.0 nM 5.41
CHEMBL237072 Ki > 5000.0 nM -
CHEMBL238362 Ki > 5000.0 nM -
CHEMBL398090 Ki - -