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Assay Detail

CHEMBL755211

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

Binding
Inhibition of [3H]DADLE radioligand binding to rat brain opioid receptor delta 1.
32
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Probes for narcotic receptor-mediated phenomena. 20. Alteration of opioid receptor subtype selectivity of the 5-(3-hydroxyphenyl)morphans by application of the message-address concept: preparation of delta-opioid receptor ligands.
Bertha CM, Flippen-Anderson JL, Rothman RB, Porreca F, Davis P, Xu H, Becketts K, Cha XY, Rice KC.
J Med Chem (1995) 38 : 1523 -1537
PubMed 7739011 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 7.18 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL340032 DADLE 1 8.77
CHEMBL290301 3 8.25
CHEMBL288803 3 8.24
CHEMBL288495 1 8.16
CHEMBL70 MORPHINE 4.0 2 8.13
CHEMBL289157 1 7.90
CHEMBL288729 1 7.75
CHEMBL39994 1 7.47
CHEMBL288730 1 7.39
CHEMBL39531 1 7.33
CHEMBL290557 1 7.16
CHEMBL38086 1 7.08
CHEMBL37584 1 6.95
CHEMBL436351 1 6.85
CHEMBL38961 1 6.74
CHEMBL290095 1 6.64
CHEMBL430732 1 6.64
CHEMBL288669 1 6.63
CHEMBL38791 3 6.56
CHEMBL39886 1 6.31
CHEMBL40188 1 5.98
CHEMBL434203 1 -
CHEMBL39319 1 -
CHEMBL285250 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL340032 DADLE IC50 = 1.71 nM 8.77
CHEMBL290301 IC50 = 5.6 nM 8.25
CHEMBL288803 IC50 = 5.7 nM 8.24
CHEMBL288803 IC50 = 6.2 nM 8.21
CHEMBL288495 IC50 = 6.9 nM 8.16
CHEMBL290301 IC50 = 7.1 nM 8.15
CHEMBL70 MORPHINE IC50 = 7.37 nM 8.13
CHEMBL289157 IC50 = 12.6 nM 7.90
CHEMBL288729 IC50 = 18.0 nM 7.75
CHEMBL39994 IC50 = 34.0 nM 7.47
CHEMBL288730 IC50 = 40.5 nM 7.39
CHEMBL39531 IC50 = 46.7 nM 7.33
CHEMBL290557 IC50 = 69.5 nM 7.16
CHEMBL38086 IC50 = 84.1 nM 7.08
CHEMBL37584 IC50 = 111.3 nM 6.95
CHEMBL436351 IC50 = 140.1 nM 6.85
CHEMBL38961 IC50 = 184.0 nM 6.74
CHEMBL430732 IC50 = 227.1 nM 6.64
CHEMBL290095 IC50 = 229.0 nM 6.64
CHEMBL288669 IC50 = 233.3 nM 6.63
CHEMBL38791 IC50 = 273.4 nM 6.56
CHEMBL39886 IC50 = 487.0 nM 6.31
CHEMBL290301 IC50 = 660.1 nM 6.18
CHEMBL70 MORPHINE IC50 = 684.0 nM 6.17
CHEMBL38791 IC50 = 720.0 nM 6.14
CHEMBL40188 IC50 = 1052.0 nM 5.98
CHEMBL38791 IC50 = 1136.0 nM 5.95
CHEMBL285250 IC50 > 1000.0 nM -
CHEMBL39319 IC50 > 10000.0 nM -
CHEMBL434203 IC50 > 1000.0 nM -
CHEMBL285250 IC50 > 1000.0 nM -
CHEMBL288803 IC50 > 1000.0 nM -