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Assay Detail

CHEMBL922697

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

Binding
Displacement of [3H]diprenorphine from recombinant delta opioid receptor expressed in C6 cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type C6
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Delta-type opioid receptor (CHEMBL236)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Opioids and efflux transporters. Part 2: P-glycoprotein substrate activity of 3- and 6-substituted morphine analogs.
Cunningham CW, Mercer SL, Hassan HE, Traynor JR, Eddington ND, Coop A.
J Med Chem (2008) 51 : 2316 -2320
PubMed 18311899 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.00 7.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL410907 1 7.93
CHEMBL358043 HETEROCODEINE 1 7.18
CHEMBL70 MORPHINE 4.0 1 6.98
CHEMBL261048 1 6.62
CHEMBL412301 1 5.36
CHEMBL408422 1 5.34
CHEMBL258669 1 5.28
CHEMBL409743 1 5.05
CHEMBL485 CODEINE 4.0 1 4.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL410907 Ki = 11.8 nM 7.93
CHEMBL358043 HETEROCODEINE Ki = 65.8 nM 7.18
CHEMBL70 MORPHINE Ki = 104.57 nM 6.98
CHEMBL261048 Ki = 241.0 nM 6.62
CHEMBL412301 Ki = 4410.0 nM 5.36
CHEMBL408422 Ki = 4520.0 nM 5.34
CHEMBL258669 Ki = 5250.0 nM 5.28
CHEMBL409743 Ki = 8830.0 nM 5.05
CHEMBL485 CODEINE Ki = 52207.0 nM 4.28