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Assay Detail

CHEMBL886502

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

Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
41
Total Activities
41
Compounds Tested
2
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

Nociceptin receptor (CHEMBL2014)
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 40 8.02 9.52
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL392798 1 9.52
CHEMBL240005 1 9.10
CHEMBL239824 1 9.05
CHEMBL391082 1 8.96
CHEMBL284414 1 8.92
CHEMBL239822 1 8.89
CHEMBL393807 1 8.85
CHEMBL27460 1 8.85
CHEMBL428033 1 8.82
CHEMBL241086 1 8.70
CHEMBL240215 1 8.64
CHEMBL241112 1 8.62
CHEMBL393781 1 8.59
CHEMBL401451 1 8.49
CHEMBL392893 1 8.46
CHEMBL391083 1 8.34
CHEMBL239820 1 8.20
CHEMBL241272 1 8.17
CHEMBL241087 1 8.08
CHEMBL439212 1 8.05
CHEMBL428563 1 8.05
CHEMBL241085 1 7.97
CHEMBL392969 1 7.97
CHEMBL203356 1 7.96
CHEMBL241079 1 7.94
CHEMBL240033 1 7.85
CHEMBL442090 1 7.84
CHEMBL393980 1 7.82
CHEMBL240216 1 7.77
CHEMBL240657 1 7.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL392798 Ki = 0.3 nM 9.52
CHEMBL240005 Ki = 0.8 nM 9.10
CHEMBL239824 Ki = 0.9 nM 9.05
CHEMBL391082 Ki = 1.1 nM 8.96
CHEMBL284414 Ki = 1.2 nM 8.92
CHEMBL239822 Ki = 1.3 nM 8.89
CHEMBL393807 Ki = 1.4 nM 8.85
CHEMBL27460 Ki = 1.4 nM 8.85
CHEMBL428033 Ki = 1.5 nM 8.82
CHEMBL241086 Ki = 2.0 nM 8.70
CHEMBL240215 Ki = 2.3 nM 8.64
CHEMBL241112 Ki = 2.4 nM 8.62
CHEMBL393781 Ki = 2.6 nM 8.59
CHEMBL401451 Ki = 3.2 nM 8.49
CHEMBL392893 Ki = 3.5 nM 8.46
CHEMBL391083 Ki = 4.6 nM 8.34
CHEMBL239820 Ki = 6.3 nM 8.20
CHEMBL241272 Ki = 6.8 nM 8.17
CHEMBL241087 Ki = 8.4 nM 8.08
CHEMBL428563 Ki = 9.0 nM 8.05
CHEMBL439212 Ki = 9.0 nM 8.05
CHEMBL241085 Ki = 10.8 nM 7.97
CHEMBL392969 Ki = 10.8 nM 7.97
CHEMBL203356 Ki = 11.0 nM 7.96
CHEMBL241079 Ki = 11.5 nM 7.94
CHEMBL240033 Ki = 14.0 nM 7.85
CHEMBL442090 Ki = 14.5 nM 7.84
CHEMBL393980 Ki = 15.1 nM 7.82
CHEMBL240216 Ki = 17.0 nM 7.77
CHEMBL240657 Ki = 23.0 nM 7.64
CHEMBL241067 Ki = 36.5 nM 7.44
CHEMBL391703 Ki = 49.0 nM 7.31
CHEMBL240001 Ki = 61.2 nM 7.21
CHEMBL240895 Ki = 119.0 nM 6.92
CHEMBL240896 Ki = 133.0 nM 6.88
CHEMBL241080 Ki = 140.0 nM 6.85
CHEMBL240870 Ki = 225.0 nM 6.65
CHEMBL239819 Ki = 249.0 nM 6.60
CHEMBL239821 Ki = 250.0 nM 6.60
CHEMBL240897 Ki = 824.0 nM 6.08
CHEMBL240869 Activity - -