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Assay Detail

CHEMBL699595

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

Binding
Binding affinity against Kappa opioid receptor using [3H]U-69593 radioligand in mouse brain homogenates
12
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Kappa-type opioid receptor (CHEMBL4329)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Pyrrolooctahydroisoquinolines as potent and selective opioid receptor ligands: SAR analysis and docking studies
Dondio G, Ronzoni S, Petrillo P, DesJarlais RL, Raveglia LF
Bioorg Med Chem Lett (1997) 7 : 2967 -2972
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.53 8.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2051964 1 8.02
CHEMBL327956 1 7.15
CHEMBL322181 1 6.77
CHEMBL327745 1 6.51
CHEMBL101516 1 6.35
CHEMBL108076 1 6.30
CHEMBL100729 3 5.89
CHEMBL100911 1 -
CHEMBL316863 1 -
CHEMBL101623 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2051964 Ki = 9.5 nM 8.02
CHEMBL327956 Ki = 70.4 nM 7.15
CHEMBL322181 Ki = 169.2 nM 6.77
CHEMBL327745 Ki = 312.0 nM 6.51
CHEMBL101516 Ki = 449.0 nM 6.35
CHEMBL108076 Ki = 500.0 nM 6.30
CHEMBL100729 Ki = 1298.0 nM 5.89
CHEMBL100729 Ki = 1340.0 nM 5.87
CHEMBL100729 Ki = 1340.0 nM 5.87
CHEMBL100911 Ki > 1000.0 nM -
CHEMBL316863 Ki > 1000.0 nM -
CHEMBL101623 Ki > 1000.0 nM -