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Assay Detail

CHEMBL966890

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

Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
48
Total Activities
45
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 Autocuration

Target

Nociceptin receptor (CHEMBL2014)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of tropane derivatives as nociceptin receptor ligands for the management of cough and anxiety.
Ho GD, Anthes J, Bercovici A, Caldwell JP, Cheng KC, Cui X, Fawzi A, Fernandez X, Greenlee WJ, Hey J, Korfmacher W, Lu SX, McLeod RL, Ng F, Torhan AS, Tan Z, Tulshian D, Varty GB, Xu X, Zhang H.
Bioorg Med Chem Lett (2009) 19 : 2519 -2523
PubMed 19339177 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 48 7.69 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL513136 1 9.52
CHEMBL512414 1 8.77
CHEMBL466067 1 8.72
CHEMBL467314 1 8.70
CHEMBL511920 1 8.64
CHEMBL467488 1 8.57
CHEMBL513471 1 8.52
CHEMBL466679 1 8.52
CHEMBL511374 1 8.52
CHEMBL466847 1 8.47
CHEMBL506634 1 8.44
CHEMBL512258 1 8.40
CHEMBL467497 1 8.31
CHEMBL512411 1 8.28
CHEMBL513660 1 8.28
CHEMBL468952 1 8.22
CHEMBL467313 1 8.22
CHEMBL513667 1 8.15
CHEMBL466126 1 8.14
CHEMBL512247 1 8.13
CHEMBL466846 1 8.12
CHEMBL512950 1 8.10
CHEMBL466693 1 8.09
CHEMBL513171 2 8.00
CHEMBL467699 1 8.00
CHEMBL466694 1 7.96
CHEMBL466919 1 7.96
CHEMBL228690 1 7.89
CHEMBL466066 1 7.89
CHEMBL513303 1 7.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL513136 Ki = 0.3 nM 9.52
CHEMBL512414 Ki = 1.7 nM 8.77
CHEMBL466067 Ki = 1.9 nM 8.72
CHEMBL467314 Ki = 2.0 nM 8.70
CHEMBL511920 Ki = 2.3 nM 8.64
CHEMBL467488 Ki = 2.7 nM 8.57
CHEMBL513471 Ki = 3.0 nM 8.52
CHEMBL466679 Ki = 3.0 nM 8.52
CHEMBL511374 Ki = 3.0 nM 8.52
CHEMBL466847 Ki = 3.4 nM 8.47
CHEMBL506634 Ki = 3.6 nM 8.44
CHEMBL512258 Ki = 4.0 nM 8.40
CHEMBL467497 Ki = 4.9 nM 8.31
CHEMBL513660 Ki = 5.3 nM 8.28
CHEMBL512411 Ki = 5.2 nM 8.28
CHEMBL467313 Ki = 6.0 nM 8.22
CHEMBL468952 Ki = 6.0 nM 8.22
CHEMBL513667 Ki = 7.0 nM 8.15
CHEMBL466126 Ki = 7.3 nM 8.14
CHEMBL512247 Ki = 7.4 nM 8.13
CHEMBL466846 Ki = 7.5 nM 8.12
CHEMBL512950 Ki = 8.0 nM 8.10
CHEMBL466693 Ki = 8.2 nM 8.09
CHEMBL513171 Ki = 10.0 nM 8.00
CHEMBL467699 Ki = 10.0 nM 8.00
CHEMBL466919 Ki = 11.0 nM 7.96
CHEMBL466694 Ki = 11.0 nM 7.96
CHEMBL228690 Ki = 13.0 nM 7.89
CHEMBL466066 Ki = 13.0 nM 7.89
CHEMBL513303 Ki = 14.0 nM 7.85
CHEMBL466921 Ki = 16.0 nM 7.80
CHEMBL511373 Ki = 19.0 nM 7.72
CHEMBL467119 Ki = 20.0 nM 7.70
CHEMBL512612 Ki = 22.0 nM 7.66
CHEMBL467131 Ki = 31.0 nM 7.51
CHEMBL511223 Ki = 40.0 nM 7.40
CHEMBL468953 Ki = 100.0 nM 7.00
CHEMBL467933 Ki = 142.0 nM 6.85
CHEMBL466438 Ki = 198.0 nM 6.70
CHEMBL466469 Ki = 285.0 nM 6.54
CHEMBL466082 Ki = 385.0 nM 6.42
CHEMBL467494 Ki = 678.0 nM 6.17
CHEMBL512982 Ki = 908.0 nM 6.04
CHEMBL466438 Ki = 1090.0 nM 5.96
CHEMBL467676 Ki = 1571.0 nM 5.80
CHEMBL511373 Ki = 2999.0 nM 5.52
CHEMBL506803 Ki = 3151.0 nM 5.50
CHEMBL513171 Ki = 3759.0 nM 5.42