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Assay Detail

CHEMBL886504

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

Binding
Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO cell membrane
41
Total Activities
41
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

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

Publication

Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands.
Caldwell JP, Matasi JJ, Zhang H, Fawzi A, Tulshian DB.
Bioorg Med Chem Lett (2007) 17 : 2281 -2284
PubMed 17289383 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 41 6.68 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL391082 1 7.89
CHEMBL240005 1 7.86
CHEMBL401451 1 7.79
CHEMBL241112 1 7.65
CHEMBL428033 1 7.59
CHEMBL391083 1 7.58
CHEMBL240033 1 7.58
CHEMBL284414 1 7.50
CHEMBL239824 1 7.47
CHEMBL392893 1 7.30
CHEMBL240215 1 7.28
CHEMBL240216 1 7.22
CHEMBL27460 1 7.19
CHEMBL241085 1 7.18
CHEMBL241086 1 7.03
CHEMBL240657 1 6.86
CHEMBL393781 1 6.84
CHEMBL392798 1 6.84
CHEMBL241087 1 6.77
CHEMBL203356 1 6.71
CHEMBL442090 1 6.69
CHEMBL240896 1 6.60
CHEMBL393807 1 6.55
CHEMBL240895 1 6.49
CHEMBL240001 1 6.29
CHEMBL239822 1 6.27
CHEMBL241079 1 6.24
CHEMBL241067 1 6.11
CHEMBL239820 1 6.07
CHEMBL393980 1 6.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL391082 Ki = 13.0 nM 7.89
CHEMBL240005 Ki = 13.7 nM 7.86
CHEMBL401451 Ki = 16.4 nM 7.79
CHEMBL241112 Ki = 22.5 nM 7.65
CHEMBL428033 Ki = 25.5 nM 7.59
CHEMBL391083 Ki = 26.0 nM 7.58
CHEMBL240033 Ki = 26.2 nM 7.58
CHEMBL284414 Ki = 32.0 nM 7.50
CHEMBL239824 Ki = 33.5 nM 7.47
CHEMBL392893 Ki = 50.0 nM 7.30
CHEMBL240215 Ki = 52.3 nM 7.28
CHEMBL240216 Ki = 60.5 nM 7.22
CHEMBL27460 Ki = 65.0 nM 7.19
CHEMBL241085 Ki = 66.5 nM 7.18
CHEMBL241086 Ki = 94.5 nM 7.03
CHEMBL240657 Ki = 137.0 nM 6.86
CHEMBL393781 Ki = 143.0 nM 6.84
CHEMBL392798 Ki = 145.0 nM 6.84
CHEMBL241087 Ki = 169.0 nM 6.77
CHEMBL203356 Ki = 196.0 nM 6.71
CHEMBL442090 Ki = 203.0 nM 6.69
CHEMBL240896 Ki = 252.0 nM 6.60
CHEMBL393807 Ki = 282.0 nM 6.55
CHEMBL240895 Ki = 321.0 nM 6.49
CHEMBL240001 Ki = 517.0 nM 6.29
CHEMBL239822 Ki = 540.0 nM 6.27
CHEMBL241079 Ki = 579.0 nM 6.24
CHEMBL241067 Ki = 776.0 nM 6.11
CHEMBL239820 Ki = 858.0 nM 6.07
CHEMBL393980 Ki = 938.0 nM 6.03
CHEMBL428563 Ki = 1086.0 nM 5.96
CHEMBL392969 Ki = 1183.0 nM 5.93
CHEMBL239821 Ki = 1448.0 nM 5.84
CHEMBL439212 Ki = 1602.0 nM 5.79
CHEMBL240870 Ki = 1672.0 nM 5.78
CHEMBL391703 Ki = 2009.0 nM 5.70
CHEMBL241080 Ki = 3529.0 nM 5.45
CHEMBL239819 Ki = 4628.0 nM 5.33
CHEMBL241272 Ki = 5887.0 nM 5.23
CHEMBL240869 Ki - -
CHEMBL240897 Ki - -