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Assay Detail

CHEMBL1001567

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

Functional
Antagonist activity at human recombinant kappa opioid receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of dynorphin A-induced intracellular calcium mobilization
2
Total Activities
2
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

Further studies at neuropeptide s position 5: discovery of novel neuropeptide S receptor antagonists.
Guerrini R, Camarda V, Trapella C, Caló G, Rizzi A, Ruzza C, Fiorini S, Marzola E, Reinscheid RK, Regoli D, Salvadori S.
J Med Chem (2009) 52 : 4068 -4071
PubMed 19473027 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 8.42 8.63

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1627325 1 8.63
CHEMBL411557 DYNORPHIN A (1-17) 1 8.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1627325 EC50 = 2.344 nM 8.63
CHEMBL411557 DYNORPHIN A (1-17) EC50 = 6.31 nM 8.20