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Assay Detail

CHEMBL900508

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

Functional
Agonist activity at human kappa opioid receptor assessed as inhibition of Galpha-16-induced calcium flux
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Synthetic studies of neoclerodane diterpenes from Salvia divinorum: exploration of the 1-position.
Holden KG, Tidgewell K, Marquam A, Rothman RB, Navarro H, Prisinzano TE.
Bioorg Med Chem Lett (2007) 17 : 6111 -6115
PubMed 17904842 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 8.68 8.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL445332 SALVINORIN A 1.0 1 8.91
CHEMBL440765 U-69593 1 8.65
CHEMBL365533 1 8.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL445332 SALVINORIN A EC50 = 1.24 nM 8.91
CHEMBL440765 U-69593 EC50 = 2.25 nM 8.65
CHEMBL365533 EC50 = 3.34 nM 8.48