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Assay Detail

CHEMBL840061

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

Binding
Inhibition of [3H]naloxone binding to rat brain homogenate Opioid receptor delta
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Delta-type opioid receptor (CHEMBL269)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

6-Hydroxy-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid mimics active conformation of tyrosine in opioid peptides.
Sperlinga E, Kosson P, Urbanczyk-Lipkowska Z, Ronsisvalle G, Carr DB, Lipkowski AW.
Bioorg Med Chem Lett (2005) 15 : 2467 -2469
PubMed 15863298 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 6.93 9.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL317956 DELTORPHIN C 1 9.14
CHEMBL191777 1 7.98
CHEMBL278789 DERMORPHIN 1 6.53
CHEMBL2371868 1 6.52
CHEMBL317264 1 5.74
CHEMBL333357 ENDOMORPHIN 2 1 5.64
CHEMBL2371865 1 -
CHEMBL2371866 1 -
CHEMBL370392 1 -
CHEMBL2371867 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL317956 DELTORPHIN C Ki = 0.73 nM 9.14
CHEMBL191777 Ki = 10.4 nM 7.98
CHEMBL278789 DERMORPHIN Ki = 295.0 nM 6.53
CHEMBL2371868 Ki = 304.0 nM 6.52
CHEMBL317264 Ki = 1820.0 nM 5.74
CHEMBL333357 ENDOMORPHIN 2 Ki = 2300.0 nM 5.64
CHEMBL2371865 Ki > 10000.0 nM -
CHEMBL2371866 Ki > 10000.0 nM -
CHEMBL370392 Ki > 10000.0 nM -
CHEMBL2371867 Ki > 10000.0 nM -