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Assay Detail

CHEMBL835443

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

Functional
Antagonist activity against deltorphin in mouse vas deferens assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Direct influence of C-terminally substituted amino acids in the Dmt-Tic pharmacophore on delta-opioid receptor selectivity and antagonism.
Balboni G, Salvadori S, Guerrini R, Negri L, Giannini E, Bryant SD, Jinsmaa Y, Lazarus LH.
J Med Chem (2004) 47 : 4066 -4071
PubMed 15267245 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 20 8.44 10.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3142535 1 10.07
CHEMBL3085298 1 9.57
CHEMBL3142536 1 9.29
CHEMBL2369957 1 8.98
CHEMBL2369978 1 8.91
CHEMBL2371781 1 8.88
CHEMBL2371780 1 8.72
CHEMBL2369981 1 8.64
CHEMBL2371813 1 8.40
CHEMBL2369980 1 8.23
CHEMBL607481 1 8.23
CHEMBL2369979 1 8.14
CHEMBL606602 1 8.12
CHEMBL2371782 1 8.07
CHEMBL606601 1 8.00
CHEMBL2371778 1 7.87
CHEMBL2371779 1 7.65
CHEMBL607402 1 7.60
CHEMBL3085297 1 6.90
CHEMBL2369958 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3142535 Kd = 0.08511 nM 10.07
CHEMBL3085298 Kd = 0.2692 nM 9.57
CHEMBL3142536 Kd = 0.5129 nM 9.29
CHEMBL2369957 Kd = 1.047 nM 8.98
CHEMBL2369978 Kd = 1.23 nM 8.91
CHEMBL2371781 Kd = 1.318 nM 8.88
CHEMBL2371780 Kd = 1.905 nM 8.72
CHEMBL2369981 Kd = 2.291 nM 8.64
CHEMBL2371813 Kd = 3.981 nM 8.40
CHEMBL2369980 Kd = 5.888 nM 8.23
CHEMBL607481 Kd = 5.888 nM 8.23
CHEMBL2369979 Kd = 7.244 nM 8.14
CHEMBL606602 Kd = 7.586 nM 8.12
CHEMBL2371782 Kd = 8.511 nM 8.07
CHEMBL606601 Kd = 10.0 nM 8.00
CHEMBL2371778 Kd = 13.49 nM 7.87
CHEMBL2371779 Kd = 22.39 nM 7.65
CHEMBL607402 Kd = 25.12 nM 7.60
CHEMBL3085297 Kd = 125.89 nM 6.90
CHEMBL2369958 Kd < 0.1 nM -