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Assay Detail

CHEMBL930987

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

Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Nociceptin receptor (CHEMBL2014)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and pharmacological evaluation of 1,2-dihydrospiro[isoquinoline-4(3H),4'-piperidin]-3-ones as nociceptin receptor agonists.
Mustazza C, Borioni A, Sestili I, Sbraccia M, Rodomonte A, Del Giudice MR.
J Med Chem (2008) 51 : 1058 -1062
PubMed 18232652 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 7.37 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL396460 NOCICEPTIN 1 9.89
CHEMBL412098 1 9.41
CHEMBL272852 1 8.51
CHEMBL271590 1 8.33
CHEMBL409621 1 8.18
CHEMBL272601 1 8.05
CHEMBL270756 1 7.92
CHEMBL272390 1 7.68
CHEMBL407846 1 7.64
CHEMBL412290 1 7.58
CHEMBL272640 1 7.38
CHEMBL272805 1 7.29
CHEMBL449966 1 7.19
CHEMBL259473 1 7.09
CHEMBL272592 1 7.05
CHEMBL272896 1 7.04
CHEMBL271779 1 7.00
CHEMBL271342 1 6.98
CHEMBL271322 1 6.89
CHEMBL259681 1 6.87
CHEMBL407275 1 6.83
CHEMBL271542 1 6.75
CHEMBL270133 1 6.73
CHEMBL406758 1 6.73
CHEMBL271187 1 6.58
CHEMBL272600 1 6.40
CHEMBL271341 1 6.26
CHEMBL271185 1 6.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL396460 NOCICEPTIN Ki = 0.13 nM 9.89
CHEMBL412098 Ki = 0.39 nM 9.41
CHEMBL272852 Ki = 3.1 nM 8.51
CHEMBL271590 Ki = 4.7 nM 8.33
CHEMBL409621 Ki = 6.6 nM 8.18
CHEMBL272601 Ki = 8.9 nM 8.05
CHEMBL270756 Ki = 12.0 nM 7.92
CHEMBL272390 Ki = 21.0 nM 7.68
CHEMBL407846 Ki = 23.0 nM 7.64
CHEMBL412290 Ki = 26.0 nM 7.58
CHEMBL272640 Ki = 42.0 nM 7.38
CHEMBL272805 Ki = 51.0 nM 7.29
CHEMBL449966 Ki = 65.0 nM 7.19
CHEMBL259473 Ki = 81.0 nM 7.09
CHEMBL272592 Ki = 90.0 nM 7.05
CHEMBL272896 Ki = 92.0 nM 7.04
CHEMBL271779 Ki = 100.0 nM 7.00
CHEMBL271342 Ki = 104.0 nM 6.98
CHEMBL271322 Ki = 130.0 nM 6.89
CHEMBL259681 Ki = 136.0 nM 6.87
CHEMBL407275 Ki = 147.0 nM 6.83
CHEMBL271542 Ki = 180.0 nM 6.75
CHEMBL270133 Ki = 186.0 nM 6.73
CHEMBL406758 Ki = 186.0 nM 6.73
CHEMBL271187 Ki = 260.0 nM 6.58
CHEMBL272600 Ki = 395.0 nM 6.40
CHEMBL271341 Ki = 545.0 nM 6.26
CHEMBL271185 Ki = 740.0 nM 6.13