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Assay Detail

CHEMBL753344

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

Binding
Binding affinity towards delta receptor in rat brain using [3H]DSLET
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Expert

Target

Delta-type opioid receptor (CHEMBL269)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Pseudoproline-containing analogues of morphiceptin and endomorphin-2: evidence for a cis Tyr-Pro amide bond in the bioactive conformation.
Keller M, Boissard C, Patiny L, Chung NN, Lemieux C, Mutter M, Schiller PW.
J Med Chem (2001) 44 : 3896 -3903
PubMed 11689075 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 6.33 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL35838 [LEU5]ENKEPHALIN 1 8.60
CHEMBL338198 1 5.70
CHEMBL126611 1 5.61
CHEMBL333357 ENDOMORPHIN 2 1 5.41
CHEMBL126794 1 -
CHEMBL338113 1 -
CHEMBL338572 1 -
CHEMBL339725 1 -
CHEMBL129323 1 -
CHEMBL339724 1 -
CHEMBL2370620 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL35838 [LEU5]ENKEPHALIN Ki = 2.53 nM 8.60
CHEMBL338198 Ki = 1980.0 nM 5.70
CHEMBL126611 Ki = 2450.0 nM 5.61
CHEMBL333357 ENDOMORPHIN 2 Ki = 3940.0 nM 5.41
CHEMBL126794 Ki > 10000.0 nM -
CHEMBL338113 Ki > 10000.0 nM -
CHEMBL338572 Ki > 10000.0 nM -
CHEMBL339725 Ki > 4000.0 nM -
CHEMBL129323 Ki > 10000.0 nM -
CHEMBL339724 Ki > 10000.0 nM -
CHEMBL2370620 Ki > 10000.0 nM -