Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL754404

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

Binding
Binding affinity to opioid receptors by the displacement of [3H]fentanyl in rat brain homogenates
27
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Opioid receptor (CHEMBL2094129)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Opiate receptor interaction of compounds derived from or structurally related to fentanyl.
Lobbezoo MW, Soudijn W, van Wijngaarden I.
J Med Chem (1981) 24 : 777 -782
PubMed 6268786 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 7.35 9.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL351642 1 9.08
CHEMBL596 FENTANYL 4.0 1 8.94
CHEMBL351213 1 8.87
CHEMBL164627 1 8.81
CHEMBL349167 1 8.79
CHEMBL167362 1 8.70
CHEMBL423089 1 8.61
CHEMBL165403 1 8.35
CHEMBL423805 1 7.99
CHEMBL353786 1 7.92
CHEMBL164876 1 7.54
CHEMBL164008 1 7.34
CHEMBL349296 1 7.21
CHEMBL164846 1 7.15
CHEMBL165143 1 7.07
CHEMBL164606 1 7.00
CHEMBL352108 1 6.96
CHEMBL349970 1 6.60
CHEMBL348917 1 6.54
CHEMBL348721 1 6.46
CHEMBL165227 1 6.31
CHEMBL354142 2 6.14
CHEMBL350864 1 6.12
CHEMBL163721 1 6.09
CHEMBL424535 1 6.01
CHEMBL164007 1 5.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL351642 IC50 = 0.84 nM 9.08
CHEMBL596 FENTANYL IC50 = 1.14 nM 8.94
CHEMBL351213 IC50 = 1.36 nM 8.87
CHEMBL164627 IC50 = 1.56 nM 8.81
CHEMBL349167 IC50 = 1.64 nM 8.79
CHEMBL167362 IC50 = 1.99 nM 8.70
CHEMBL423089 IC50 = 2.48 nM 8.61
CHEMBL165403 IC50 = 4.48 nM 8.35
CHEMBL423805 IC50 = 10.2 nM 7.99
CHEMBL353786 IC50 = 11.9 nM 7.92
CHEMBL164876 IC50 = 29.0 nM 7.54
CHEMBL164008 IC50 = 46.0 nM 7.34
CHEMBL349296 IC50 = 61.0 nM 7.21
CHEMBL164846 IC50 = 71.0 nM 7.15
CHEMBL165143 IC50 = 86.0 nM 7.07
CHEMBL164606 IC50 = 101.0 nM 7.00
CHEMBL352108 IC50 = 109.0 nM 6.96
CHEMBL349970 IC50 = 250.0 nM 6.60
CHEMBL348917 IC50 = 290.0 nM 6.54
CHEMBL348721 IC50 = 345.0 nM 6.46
CHEMBL165227 IC50 = 490.0 nM 6.31
CHEMBL354142 IC50 = 721.0 nM 6.14
CHEMBL350864 IC50 = 767.0 nM 6.12
CHEMBL163721 IC50 = 810.0 nM 6.09
CHEMBL354142 IC50 = 889.0 nM 6.05
CHEMBL424535 IC50 = 980.0 nM 6.01
CHEMBL164007 IC50 = 2140.0 nM 5.67