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Assay Detail

CHEMBL1055015

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Functional
Antagonist activity against delta opioid receptor in mouse vas deferens assessed as effect on deltorphin 2-induced contraction
16
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Tissue Vas deferens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Delta-type opioid receptor (CHEMBL3222)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Influence of the side chain next to C-terminal benzimidazole in opioid pseudopeptides containing the Dmt-Tic pharmacophore.
Balboni G, Trapella C, Sasaki Y, Ambo A, Marczak ED, Lazarus LH, Salvadori S.
J Med Chem (2009) 52 : 5556 -5559
PubMed 19642675 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
pA2 10 - -
Kd 6 8.81 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL555206 1 9.70
CHEMBL538700 1 9.68
CHEMBL556063 1 8.79
CHEMBL554625 1 8.60
CHEMBL191751 1 8.32
CHEMBL557035 1 7.74
CHEMBL538456 1 -
CHEMBL538457 1 -
CHEMBL539386 1 -
CHEMBL564083 1 -
CHEMBL554838 1 -
CHEMBL538699 1 -
CHEMBL538384 1 -
CHEMBL557346 1 -
CHEMBL553461 1 -
CHEMBL540724 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL555206 Kd = 0.1995 nM 9.70
CHEMBL538700 Kd = 0.2089 nM 9.68
CHEMBL556063 Kd = 1.622 nM 8.79
CHEMBL554625 Kd = 2.512 nM 8.60
CHEMBL191751 Kd = 4.786 nM 8.32
CHEMBL557035 Kd = 18.2 nM 7.74
CHEMBL538456 pA2 - -
CHEMBL538457 pA2 - -
CHEMBL539386 pA2 - -
CHEMBL564083 pA2 - -
CHEMBL554838 pA2 - -
CHEMBL538699 pA2 - -
CHEMBL538384 pA2 - -
CHEMBL557346 pA2 - -
CHEMBL553461 pA2 - -
CHEMBL540724 pA2 - -