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Assay Detail

CHEMBL756077

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

Binding
Inhibition of [3H]- U69,593 binding to Guinea pig Opioid receptor kappa 1
13
Total Activities
11
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. 21. Novel derivatives of 3-(1,2,3,4,5,11-hexahydro-3-methyl-2,6-methano-6H-azocino[4,5-b]indol- 6-yl)-phenols with improved delta opioid receptor selectivity.
Bertha CM, Ellis M, Flippen-Anderson JL, Porreca F, Rothman RB, Davis P, Xu H, Becketts K, Rice KC.
J Med Chem (1996) 39 : 2081 -2086
PubMed 8642567 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.15 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL140050 ETORPHINE 2.0 1 8.74
CHEMBL70 MORPHINE 4.0 1 6.57
CHEMBL2111530 1 5.93
CHEMBL302454 2 5.75
CHEMBL340032 DADLE 1 5.36
CHEMBL38791 1 5.29
CHEMBL303113 1 -
CHEMBL65348 2 -
CHEMBL290301 1 -
CHEMBL13470 SNC-80 1 -
CHEMBL440123 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL140050 ETORPHINE IC50 = 1.82 nM 8.74
CHEMBL70 MORPHINE IC50 = 271.0 nM 6.57
CHEMBL2111530 IC50 = 1162.0 nM 5.93
CHEMBL302454 IC50 = 1770.0 nM 5.75
CHEMBL302454 IC50 = 3959.0 nM 5.40
CHEMBL340032 DADLE IC50 = 4404.0 nM 5.36
CHEMBL38791 IC50 = 5071.0 nM 5.29
CHEMBL303113 IC50 > 10000.0 nM -
CHEMBL65348 IC50 > 1000.0 nM -
CHEMBL290301 IC50 > 1000.0 nM -
CHEMBL13470 SNC-80 IC50 > 1000.0 nM -
CHEMBL65348 IC50 > 2500.0 nM -
CHEMBL440123 IC50 > 1000.0 nM -