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Assay Detail

CHEMBL753145

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Binding
Binding affinity towards opioid receptor kappa was determined
16
Total Activities
16
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 (CHEMBL237)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Highly selective kappa-opioid analgesics. 2. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide derivatives.
Halfpenny PR, Hill RG, Horwell DC, Hughes J, Hunter JC, Johnson S, Rees DC.
J Med Chem (1989) 32 : 1620 -1626
PubMed 2567782 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.74 8.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL544960 1 8.43
CHEMBL541804 1 8.15
CHEMBL555100 1 7.77
CHEMBL556414 1 7.75
CHEMBL536550 1 7.03
CHEMBL558227 1 6.84
CHEMBL553010 1 6.81
CHEMBL553665 1 6.75
CHEMBL540277 1 6.75
CHEMBL545654 1 6.58
CHEMBL43104 1 6.09
CHEMBL542102 1 5.70
CHEMBL555649 1 5.09
CHEMBL554205 1 4.60
CHEMBL2094047 1 -
CHEMBL2093981 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL544960 Ki = 3.7 nM 8.43
CHEMBL541804 Ki = 7.0 nM 8.15
CHEMBL555100 Ki = 17.0 nM 7.77
CHEMBL556414 Ki = 18.0 nM 7.75
CHEMBL536550 Ki = 94.0 nM 7.03
CHEMBL558227 Ki = 146.0 nM 6.84
CHEMBL553010 Ki = 154.0 nM 6.81
CHEMBL553665 Ki = 180.0 nM 6.75
CHEMBL540277 Ki = 180.0 nM 6.75
CHEMBL545654 Ki = 261.0 nM 6.58
CHEMBL43104 Ki = 816.0 nM 6.09
CHEMBL542102 Ki = 2000.0 nM 5.70
CHEMBL555649 Ki = 8100.0 nM 5.09
CHEMBL554205 Ki = 25000.0 nM 4.60
CHEMBL2094047 Ki > 10000.0 nM -
CHEMBL2093981 Ki > 1000.0 nM -