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Assay Detail

CHEMBL755960

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

Binding
Binding affinity for the Opioid receptor mu 1
33
Total Activities
31
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

Mu-type opioid receptor (CHEMBL4354)
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 6.23 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279968 ETHYLKETOCYCLAZOCINE 1 8.77
CHEMBL70 MORPHINE 4.0 1 8.74
CHEMBL558979 1 7.58
CHEMBL440765 U-69593 1 7.28
CHEMBL536937 1 7.09
CHEMBL557426 1 6.85
CHEMBL537165 1 6.72
CHEMBL539582 1 6.68
CHEMBL536939 1 6.46
CHEMBL544960 2 6.39
CHEMBL556957 1 6.34
CHEMBL541619 1 6.21
CHEMBL535801 1 6.14
CHEMBL537169 1 6.09
CHEMBL538309 1 6.06
CHEMBL290543 1 6.06
CHEMBL558608 2 5.85
CHEMBL534684 1 5.70
CHEMBL538308 1 5.62
CHEMBL354548 1 5.54
CHEMBL537616 1 5.48
CHEMBL559217 1 5.46
CHEMBL535581 1 5.44
CHEMBL556547 1 5.40
CHEMBL118865 SPIRADOLINE 2.0 1 5.19
CHEMBL537615 1 5.10
CHEMBL535133 1 4.75
CHEMBL535803 1 -
CHEMBL559214 1 -
CHEMBL535130 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279968 ETHYLKETOCYCLAZOCINE Ki = 1.7 nM 8.77
CHEMBL70 MORPHINE Ki = 1.8 nM 8.74
CHEMBL558979 Ki = 26.0 nM 7.58
CHEMBL440765 U-69593 Ki = 52.0 nM 7.28
CHEMBL536937 Ki = 81.0 nM 7.09
CHEMBL557426 Ki = 140.0 nM 6.85
CHEMBL537165 Ki = 190.0 nM 6.72
CHEMBL539582 Ki = 210.0 nM 6.68
CHEMBL536939 Ki = 350.0 nM 6.46
CHEMBL544960 Ki = 410.0 nM 6.39
CHEMBL556957 Ki = 460.0 nM 6.34
CHEMBL541619 Ki = 620.0 nM 6.21
CHEMBL535801 Ki = 720.0 nM 6.14
CHEMBL537169 Ki = 810.0 nM 6.09
CHEMBL538309 Ki = 880.0 nM 6.06
CHEMBL290543 Ki = 880.0 nM 6.06
CHEMBL544960 Ki = 1000.0 nM 6.00
CHEMBL558608 Ki = 1400.0 nM 5.85
CHEMBL558608 Ki = 1600.0 nM 5.80
CHEMBL534684 Ki = 2000.0 nM 5.70
CHEMBL538308 Ki = 2400.0 nM 5.62
CHEMBL354548 Ki = 2900.0 nM 5.54
CHEMBL537616 Ki = 3300.0 nM 5.48
CHEMBL559217 Ki = 3500.0 nM 5.46
CHEMBL535581 Ki = 3600.0 nM 5.44
CHEMBL556547 Ki = 4000.0 nM 5.40
CHEMBL118865 SPIRADOLINE Ki = 6400.0 nM 5.19
CHEMBL537615 Ki = 7900.0 nM 5.10
CHEMBL535133 Ki = 18000.0 nM 4.75
CHEMBL559214 Ki > 1000.0 nM -
CHEMBL556802 Ki > 1000.0 nM -
CHEMBL535803 Ki > 10000.0 nM -
CHEMBL535130 Ki > 1000.0 nM -