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Assay Detail

CHEMBL4701856

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

Binding
Displacement of [3H]-Diprenorphine from recombinant human delta opioid receptor expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Delta-type opioid receptor (CHEMBL236)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimized Opioid-Neurotensin Multitarget Peptides: From Design to Structure-Activity Relationship Studies.
Gonzalez S,Dumitrascuta M,Eiselt E,Louis S,Kunze L,Blasiol A,Vivancos M,Previti S,Dewolf E,Martin C,Tourwé D,Cavelier F,Gendron L,Sarret P,Spetea M,Ballet S
J Med Chem (2020) 63 : 12929 -12941
PubMed 32902268 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.11 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3408737 1 8.82
CHEMBL4761165 1 7.33
CHEMBL4749016 1 7.31
CHEMBL4789659 1 7.25
CHEMBL4745899 1 7.21
CHEMBL4776986 1 7.00
CHEMBL4742666 1 6.98
CHEMBL4798887 1 6.80
CHEMBL4747286 1 6.70
CHEMBL4750783 1 6.68
CHEMBL4744531 1 6.67
CHEMBL4758754 1 6.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3408737 Ki = 1.51 nM 8.82
CHEMBL4761165 Ki = 46.4 nM 7.33
CHEMBL4749016 Ki = 48.6 nM 7.31
CHEMBL4789659 Ki = 56.4 nM 7.25
CHEMBL4745899 Ki = 60.9 nM 7.21
CHEMBL4776986 Ki = 101.0 nM 7.00
CHEMBL4742666 Ki = 105.0 nM 6.98
CHEMBL4798887 Ki = 159.0 nM 6.80
CHEMBL4747286 Ki = 200.0 nM 6.70
CHEMBL4750783 Ki = 209.0 nM 6.68
CHEMBL4744531 Ki = 213.0 nM 6.67
CHEMBL4758754 Ki = 276.0 nM 6.56