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Assay Detail

CHEMBL5511983

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Functional
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
11
Total Activities
11
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
IC50 11 8.05 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL340032 DADLE 1 10.40
CHEMBL3303774 1 9.10
CHEMBL5568330 1 8.76
CHEMBL2364605 CEBRANOPADOL 3.0 1 8.42
CHEMBL5542870 1 7.63
CHEMBL4467777 1 6.96
CHEMBL596 FENTANYL 4.0 1 6.82
CHEMBL70 MORPHINE 4.0 1 6.28
CHEMBL573214 NORBINALTORPHIMINE 1 -
CHEMBL396460 NOCICEPTIN 1 -
CHEMBL290543 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL340032 DADLE IC50 = 0.04 nM 10.40
CHEMBL3303774 IC50 = 0.79 nM 9.10
CHEMBL5568330 IC50 = 1.75 nM 8.76
CHEMBL2364605 CEBRANOPADOL IC50 = 3.77 nM 8.42
CHEMBL5542870 IC50 = 23.51 nM 7.63
CHEMBL4467777 IC50 = 108.4 nM 6.96
CHEMBL596 FENTANYL IC50 = 150.03 nM 6.82
CHEMBL70 MORPHINE IC50 = 524.84 nM 6.28
CHEMBL573214 NORBINALTORPHIMINE IC50 - -
CHEMBL396460 NOCICEPTIN IC50 - -
CHEMBL290543 IC50 - -