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Assay Detail

CHEMBL754735

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Binding
Binding affinity for the Opioid receptor kappa 1
33
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Kappa-type opioid receptor (CHEMBL3952)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Highly selective kappa opioid analgesics. Synthesis and structure-activity relationships of novel N-[(2-aminocyclohexyl)aryl]acetamide and N-[(2-aminocyclohexyl)aryloxy]acetamide derivatives.
Clark CR, Halfpenny PR, Hill RG, Horwell DC, Hughes J, Jarvis TC, Rees DC, Schofield D.
J Med Chem (1988) 31 : 831 -836
PubMed 2832603 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 7.29 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL538309 1 8.51
CHEMBL544960 3 8.43
CHEMBL556957 1 8.40
CHEMBL537616 1 8.38
CHEMBL535581 1 8.25
CHEMBL535801 1 8.19
CHEMBL440765 U-69593 1 8.14
CHEMBL290543 1 8.00
CHEMBL557426 1 7.92
CHEMBL558608 2 7.92
CHEMBL118865 SPIRADOLINE 2.0 1 7.77
CHEMBL559217 1 7.54
CHEMBL558979 1 7.52
CHEMBL541619 1 7.46
CHEMBL537169 1 7.40
CHEMBL539582 1 7.28
CHEMBL537615 1 7.14
CHEMBL354548 1 7.13
CHEMBL536937 1 7.09
CHEMBL70 MORPHINE 4.0 1 7.07
CHEMBL535130 1 6.82
CHEMBL537165 1 6.70
CHEMBL538308 1 6.60
CHEMBL534684 1 6.52
CHEMBL556802 1 6.44
CHEMBL535133 1 6.14
CHEMBL536939 1 5.75
CHEMBL556547 1 5.68
CHEMBL559214 1 -
CHEMBL535803 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL538309 Ki = 3.1 nM 8.51
CHEMBL544960 Ki = 3.7 nM 8.43
CHEMBL556957 Ki = 4.0 nM 8.40
CHEMBL537616 Ki = 4.2 nM 8.38
CHEMBL535581 Ki = 5.6 nM 8.25
CHEMBL535801 Ki = 6.4 nM 8.19
CHEMBL440765 U-69593 Ki = 7.3 nM 8.14
CHEMBL544960 Ki = 9.6 nM 8.02
CHEMBL290543 Ki = 10.0 nM 8.00
CHEMBL557426 Ki = 12.0 nM 7.92
CHEMBL558608 Ki = 12.0 nM 7.92
CHEMBL118865 SPIRADOLINE Ki = 17.0 nM 7.77
CHEMBL559217 Ki = 29.0 nM 7.54
CHEMBL558979 Ki = 30.0 nM 7.52
CHEMBL541619 Ki = 35.0 nM 7.46
CHEMBL537169 Ki = 40.0 nM 7.40
CHEMBL539582 Ki = 52.0 nM 7.28
CHEMBL537615 Ki = 72.0 nM 7.14
CHEMBL354548 Ki = 74.0 nM 7.13
CHEMBL536937 Ki = 82.0 nM 7.09
CHEMBL70 MORPHINE Ki = 86.0 nM 7.07
CHEMBL535130 Ki = 150.0 nM 6.82
CHEMBL537165 Ki = 200.0 nM 6.70
CHEMBL538308 Ki = 250.0 nM 6.60
CHEMBL534684 Ki = 300.0 nM 6.52
CHEMBL556802 Ki = 360.0 nM 6.44
CHEMBL535133 Ki = 720.0 nM 6.14
CHEMBL544960 Ki = 1500.0 nM 5.82
CHEMBL558608 Ki = 1500.0 nM 5.82
CHEMBL536939 Ki = 1800.0 nM 5.75
CHEMBL556547 Ki = 2100.0 nM 5.68
CHEMBL559214 Ki > 1000.0 nM -
CHEMBL535803 Ki > 10000.0 nM -