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Assay Detail

CHEMBL752593

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

Binding
Inhibition of [3H]U-69593 radioligand binding to Guinea pig opioid receptor kappa 1.
28
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Kappa-type opioid receptor (CHEMBL3952)
Type SINGLE PROTEIN
Organism Cavia porcellus

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 28 6.20 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70 MORPHINE 4.0 1 8.74
CHEMBL38961 1 7.05
CHEMBL290095 1 6.71
CHEMBL37584 1 6.62
CHEMBL434203 1 6.10
CHEMBL285250 2 6.09
CHEMBL38086 1 6.03
CHEMBL38791 3 6.01
CHEMBL288495 1 6.00
CHEMBL436351 1 5.67
CHEMBL430732 1 5.65
CHEMBL39886 1 5.25
CHEMBL288730 1 -
CHEMBL39994 1 -
CHEMBL39319 1 -
CHEMBL40188 1 -
CHEMBL39531 1 -
CHEMBL290557 1 -
CHEMBL290301 1 -
CHEMBL288803 3 -
CHEMBL288669 1 -
CHEMBL289157 1 -
CHEMBL288729 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70 MORPHINE IC50 = 1.82 nM 8.74
CHEMBL38961 IC50 = 90.0 nM 7.05
CHEMBL290095 IC50 = 197.0 nM 6.71
CHEMBL37584 IC50 = 240.5 nM 6.62
CHEMBL434203 IC50 = 798.3 nM 6.10
CHEMBL285250 IC50 = 818.6 nM 6.09
CHEMBL285250 IC50 = 910.5 nM 6.04
CHEMBL38086 IC50 = 934.0 nM 6.03
CHEMBL38791 IC50 = 981.5 nM 6.01
CHEMBL288495 IC50 = 993.0 nM 6.00
CHEMBL38791 IC50 = 2025.7 nM 5.69
CHEMBL436351 IC50 = 2160.0 nM 5.67
CHEMBL430732 IC50 = 2216.0 nM 5.65
CHEMBL38791 IC50 = 5071.0 nM 5.29
CHEMBL39886 IC50 = 5563.0 nM 5.25
CHEMBL40188 IC50 > 1000.0 nM -
CHEMBL288730 IC50 > 1000.0 nM -
CHEMBL39531 IC50 > 1000.0 nM -
CHEMBL39319 IC50 > 1000.0 nM -
CHEMBL288803 IC50 > 1000.0 nM -
CHEMBL290557 IC50 > 10000.0 nM -
CHEMBL290301 IC50 > 1000.0 nM -
CHEMBL288803 IC50 > 1000.0 nM -
CHEMBL288803 IC50 > 1000.0 nM -
CHEMBL39994 IC50 > 1000.0 nM -
CHEMBL288669 IC50 > 1000.0 nM -
CHEMBL289157 IC50 > 1000.0 nM -
CHEMBL288729 IC50 > 1000.0 nM -