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Assay Detail

CHEMBL839686

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

Binding
Inhibition of [3H]deltorphin II binding to delta and kappa opioid receptors expressed in HEK 293 cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Opioid receptors; delta & kappa (CHEMBL2095151)
Type SELECTIVITY GROUP
Organism Homo sapiens

Publication

A bivalent ligand (KDAN-18) containing delta-antagonist and kappa-agonist pharmacophores bridges delta2 and kappa1 opioid receptor phenotypes.
Daniels DJ, Kulkarni A, Xie Z, Bhushan RG, Portoghese PS.
J Med Chem (2005) 48 : 1713 -1716
PubMed 15771416 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 9.36 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL610614 1 9.82
CHEMBL611406 1 9.37
CHEMBL611143 1 9.28
CHEMBL610615 1 8.97
CHEMBL367889 1 -
CHEMBL175969 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL610614 Ki = 0.15 nM 9.82
CHEMBL611406 Ki = 0.43 nM 9.37
CHEMBL611143 Ki = 0.52 nM 9.28
CHEMBL610615 Ki = 1.07 nM 8.97
CHEMBL367889 Ki > 1000.0 nM -
CHEMBL175969 Ki > 1000.0 nM -