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Assay Detail

CHEMBL4051335

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Functional
Agonist activity at human kappa-type opioid receptor expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation after 30 mins in presence of forskolin by luminescence-based HitHunter cAMP assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Addressing Structural Flexibility at the A-Ring on Salvinorin A: Discovery of a Potent Kappa-Opioid Agonist with Enhanced Metabolic Stability.
Sherwood AM, Crowley RS, Paton KF, Biggerstaff A, Neuenswander B, Day VW, Kivell BM, Prisinzano TE.
J Med Chem (2017) 60 : 3866 -3878
PubMed 28376298 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 8.48 9.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL445332 SALVINORIN A 1.0 1 9.68
CHEMBL4083444 1 9.22
CHEMBL424698 SALVINORIN B 1 8.62
CHEMBL4093687 1 7.93
CHEMBL4094854 1 7.89
CHEMBL4075281 1 7.52
CHEMBL4076437 1 -
CHEMBL4086641 1 -
CHEMBL4105286 1 -
CHEMBL1257853 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL445332 SALVINORIN A EC50 = 0.21 nM 9.68
CHEMBL4083444 EC50 = 0.6 nM 9.22
CHEMBL424698 SALVINORIN B EC50 = 2.4 nM 8.62
CHEMBL4093687 EC50 = 11.7 nM 7.93
CHEMBL4094854 EC50 = 13.0 nM 7.89
CHEMBL4075281 EC50 = 30.0 nM 7.52
CHEMBL4076437 EC50 > 10000.0 nM -
CHEMBL4086641 EC50 > 10000.0 nM -
CHEMBL4105286 EC50 > 10000.0 nM -
CHEMBL1257853 EC50 > 10000.0 nM -