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Assay Detail

CHEMBL750214

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

Binding
Displacement of [3H]DSLET from rat brain membrane opioid receptor delta
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Conformational restriction of the phenylalanine residue in a cyclic opioid peptide analogue: effects on receptor selectivity and stereospecificity.
Schiller PW, Weltrowska G, Nguyen TM, Lemieux C, Chung NN, Marsden BJ, Wilkes BC.
J Med Chem (1991) 34 : 3125 -3132
PubMed 1656045 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 6.54 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL15595 1 8.60
CHEMBL107580 1 8.49
CHEMBL323024 1 8.04
CHEMBL321335 1 7.81
CHEMBL263021 1 7.29
CHEMBL325810 1 7.26
CHEMBL106849 1 6.68
CHEMBL3037875 1 5.80
CHEMBL105453 1 5.58
CHEMBL3084310 1 5.46
CHEMBL104838 1 4.89
CHEMBL105568 1 4.85
CHEMBL107906 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL15595 Ki = 2.53 nM 8.60
CHEMBL107580 Ki = 3.21 nM 8.49
CHEMBL323024 Ki = 9.22 nM 8.04
CHEMBL321335 Ki = 15.4 nM 7.81
CHEMBL263021 Ki = 50.7 nM 7.29
CHEMBL325810 Ki = 54.6 nM 7.26
CHEMBL106849 Ki = 209.0 nM 6.68
CHEMBL3037875 Ki = 1570.0 nM 5.80
CHEMBL105453 Ki = 2600.0 nM 5.58
CHEMBL3084310 Ki = 3510.0 nM 5.46
CHEMBL104838 Ki = 12800.0 nM 4.89
CHEMBL105568 Ki = 14000.0 nM 4.85
CHEMBL107906 Ki = 50100.0 nM 4.30