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Assay Detail

CHEMBL5365897

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

Functional
Agonist activity at human mu opioid receptor stably transfected in CHO cells by cAMP assay
25
Total Activities
25
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

Mu-type opioid receptor (CHEMBL233)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel series of tunable µOR modulators with enhanced brain penetration for the treatment of opioid use disorder, pain and neuropsychiatric indications.
Nerurkar A, Nguyen T, Wang S, Bhatt U, Li K, Li Y, Ding P, Seidl FJ, Holan M, Lee J, Widjaja T, Wei ZL, Sadlowski C, Sperandio D, McGee LR, Youngblood B, Schwartz N, Gehlert D, Medina JC.
Bioorg Med Chem Lett (2023) 92 : 129405 -129405
PubMed 37414346 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 25 7.54 9.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5411716 1 9.48
CHEMBL5422389 1 9.06
CHEMBL5407881 1 8.70
CHEMBL5433189 1 8.14
CHEMBL5437684 1 8.12
CHEMBL4467777 1 7.89
CHEMBL5434293 1 7.84
CHEMBL5399232 1 7.68
CHEMBL5410817 1 7.54
CHEMBL5422499 1 7.21
CHEMBL5412978 1 6.98
CHEMBL5409642 1 6.75
CHEMBL5409840 1 6.61
CHEMBL5403495 1 6.46
CHEMBL5419159 1 6.11
CHEMBL5435875 1 6.02
CHEMBL5414957 1 -
CHEMBL5397104 1 -
CHEMBL5429557 1 -
CHEMBL5424587 1 -
CHEMBL5405925 1 -
CHEMBL5421526 1 -
CHEMBL5435711 1 -
CHEMBL5403243 1 -
CHEMBL5407379 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5411716 EC50 = 0.33 nM 9.48
CHEMBL5422389 EC50 = 0.87 nM 9.06
CHEMBL5407881 EC50 = 2.0 nM 8.70
CHEMBL5433189 EC50 = 7.3 nM 8.14
CHEMBL5437684 EC50 = 7.5 nM 8.12
CHEMBL4467777 EC50 = 13.0 nM 7.89
CHEMBL5434293 EC50 = 14.5 nM 7.84
CHEMBL5399232 EC50 = 21.0 nM 7.68
CHEMBL5410817 EC50 = 29.0 nM 7.54
CHEMBL5422499 EC50 = 62.0 nM 7.21
CHEMBL5412978 EC50 = 104.0 nM 6.98
CHEMBL5409642 EC50 = 180.0 nM 6.75
CHEMBL5409840 EC50 = 243.0 nM 6.61
CHEMBL5403495 EC50 = 346.0 nM 6.46
CHEMBL5419159 EC50 = 770.0 nM 6.11
CHEMBL5435875 EC50 = 950.0 nM 6.02
CHEMBL5414957 EC50 > 3000.0 nM -
CHEMBL5397104 EC50 > 3000.0 nM -
CHEMBL5429557 EC50 > 3000.0 nM -
CHEMBL5424587 EC50 > 3000.0 nM -
CHEMBL5405925 EC50 > 3000.0 nM -
CHEMBL5421526 EC50 > 3000.0 nM -
CHEMBL5435711 EC50 > 3000.0 nM -
CHEMBL5403243 EC50 > 3000.0 nM -
CHEMBL5407379 EC50 > 3000.0 nM -