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Assay Detail

CHEMBL827945

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

Binding
Inhibitory constant against human Opioid receptor mu 1 using [3H]diprenorphine as radio ligand
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Mu-type opioid receptor (CHEMBL233)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Arylacetamide kappa opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity.
Le Bourdonnec B, Ajello CW, Seida PR, Susnow RG, Cassel JA, Belanger S, Stabley GJ, DeHaven RN, DeHaven-Hudkins DL, Dolle RE.
Bioorg Med Chem Lett (2005) 15 : 2647 -2652
PubMed 15863335 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 6.25 7.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38576 ICI-199,441 1 7.28
CHEMBL363718 1 7.13
CHEMBL191987 1 6.98
CHEMBL425897 1 6.82
CHEMBL192718 1 6.50
CHEMBL189683 1 6.36
CHEMBL189643 1 6.32
CHEMBL364907 1 6.24
CHEMBL192998 1 6.15
CHEMBL189430 1 6.11
CHEMBL190600 1 6.06
CHEMBL190766 1 5.99
CHEMBL362741 1 5.98
CHEMBL363822 1 5.98
CHEMBL190353 1 5.97
CHEMBL370538 1 5.97
CHEMBL447185 1 5.96
CHEMBL539685 1 5.91
CHEMBL190030 1 5.72
CHEMBL192734 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38576 ICI-199,441 Ki = 53.0 nM 7.28
CHEMBL363718 Ki = 74.0 nM 7.13
CHEMBL191987 Ki = 105.0 nM 6.98
CHEMBL425897 Ki = 151.0 nM 6.82
CHEMBL192718 Ki = 319.0 nM 6.50
CHEMBL189683 Ki = 440.0 nM 6.36
CHEMBL189643 Ki = 478.0 nM 6.32
CHEMBL364907 Ki = 570.0 nM 6.24
CHEMBL192998 Ki = 703.0 nM 6.15
CHEMBL189430 Ki = 785.0 nM 6.11
CHEMBL190600 Ki = 878.0 nM 6.06
CHEMBL190766 Ki = 1026.0 nM 5.99
CHEMBL362741 Ki = 1050.0 nM 5.98
CHEMBL363822 Ki = 1050.0 nM 5.98
CHEMBL190353 Ki = 1080.0 nM 5.97
CHEMBL370538 Ki = 1062.0 nM 5.97
CHEMBL447185 Ki = 1100.0 nM 5.96
CHEMBL539685 Ki = 1240.0 nM 5.91
CHEMBL190030 Ki = 1900.0 nM 5.72
CHEMBL192734 Ki = 2300.0 nM 5.64