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Assay Detail

CHEMBL3363134

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Functional
Agonist activity at human kappa opioid receptor expressed CHO cells co-expressing Galphaq16 assessed as calcium mobilization by fluorescence assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Kappa-type opioid receptor (CHEMBL237)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Studies toward the Development of Antiproliferative Neoclerodanes from Salvinorin A.
Vasiljevik T, Groer CE, Lehner K, Navarro H, Prisinzano TE.
J Nat Prod (2014) 77 : 1817 -1824
PubMed 25075762 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 7.19 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL445332 SALVINORIN A 1.0 1 8.77
CHEMBL3331545 1 5.60
CHEMBL3331546 1 -
CHEMBL3331547 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL445332 SALVINORIN A EC50 = 1.7 nM 8.77
CHEMBL3331545 EC50 = 2500.0 nM 5.60
CHEMBL3331546 EC50 > 10000.0 nM -
CHEMBL3331547 EC50 > 10000.0 nM -