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Assay Detail

CHEMBL752653

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Binding
Evaluated for the binding affinity at kappa receptor
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Kappa-type opioid receptor (CHEMBL4329)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Selective kappa-opioid agonists: synthesis and structure-activity relationships of piperidines incorporating on oxo-containing acyl group.
Giardina G, Clarke GD, Dondio G, Petrone G, Sbacchi M, Vecchietti V.
J Med Chem (1994) 37 : 3482 -3491
PubMed 7932577 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.95 9.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL433508 1 9.19
CHEMBL117008 1 9.09
CHEMBL118865 SPIRADOLINE 2.0 1 8.95
CHEMBL117370 1 8.39
CHEMBL326553 1 8.26
CHEMBL117782 1 8.25
CHEMBL326540 1 8.21
CHEMBL333621 1 8.18
CHEMBL116262 1 8.12
CHEMBL332390 1 8.10
CHEMBL117859 1 7.99
CHEMBL115800 1 7.72
CHEMBL119162 1 7.70
CHEMBL116630 1 7.65
CHEMBL326304 1 7.52
CHEMBL331716 1 7.46
CHEMBL119524 1 7.33
CHEMBL324119 1 7.28
CHEMBL119473 1 7.09
CHEMBL70 MORPHINE 4.0 1 6.52
CHEMBL326957 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL433508 Ki = 0.64 nM 9.19
CHEMBL117008 Ki = 0.81 nM 9.09
CHEMBL118865 SPIRADOLINE Ki = 1.13 nM 8.95
CHEMBL117370 Ki = 4.07 nM 8.39
CHEMBL326553 Ki = 5.44 nM 8.26
CHEMBL117782 Ki = 5.61 nM 8.25
CHEMBL326540 Ki = 6.24 nM 8.21
CHEMBL333621 Ki = 6.54 nM 8.18
CHEMBL116262 Ki = 7.6 nM 8.12
CHEMBL332390 Ki = 7.93 nM 8.10
CHEMBL117859 Ki = 10.3 nM 7.99
CHEMBL115800 Ki = 19.2 nM 7.72
CHEMBL119162 Ki = 20.0 nM 7.70
CHEMBL116630 Ki = 22.2 nM 7.65
CHEMBL326304 Ki = 30.4 nM 7.52
CHEMBL331716 Ki = 34.8 nM 7.46
CHEMBL119524 Ki = 47.0 nM 7.33
CHEMBL324119 Ki = 52.1 nM 7.28
CHEMBL119473 Ki = 80.3 nM 7.09
CHEMBL70 MORPHINE Ki = 301.0 nM 6.52
CHEMBL326957 Ki > 100.0 nM -