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Assay Detail

CHEMBL5511977

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

Functional
Partial agonist activity at human DOR expressed in CHO-K1 cells assessed as decrease in cAMP level incubated for 30 mins in presence of forskolin by HitHunter cAMP analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Delta-type opioid receptor (CHEMBL236)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Searching for Synthetic Opioid Rescue Agents: Identification of a Potent Opioid Agonist with Reduced Respiratory Depression.
Vu LY, Luo D, Johnson K, Denehy ED, Songrady JC, Martin J, Trivedi R, Alsum AR, Shaykin JD, Chaudhary CL, Woloshin EJ, Kornberger L, Bhuiyan N, Parkin S, Jiang Q, Che T, Alilain W, Turner JR, Bardo MT, Prisinzano TE.
J Med Chem (2024) 67 : 9173 -9193
PubMed 38810170 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 8.83 9.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL511142 BUPRENORPHINE 4.0 1 9.07
CHEMBL5568344 1 8.75
CHEMBL5523416 1 8.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL511142 BUPRENORPHINE EC50 = 0.85 nM 9.07
CHEMBL5568344 EC50 = 1.77 nM 8.75
CHEMBL5523416 EC50 = 2.18 nM 8.66