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Assay Detail

CHEMBL5316893

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

Binding
Binding affinity to mouse mu opioid receptor expressed in CHO cell membrane assessed as inhibition constant incubated for 1.5 hrs by competitive radioligand binding assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type CHO
Subcellular Cell membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mu-type opioid receptor (CHEMBL2858)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Structural Alterations of the "Address" Moiety of NAN Leading to the Discovery of a Novel Opioid Receptor Modulator with Reduced hERG Toxicity.
Ma H, Pagare PP, Li M, Neel LT, Mendez RE, Gillespie JC, Stevens DL, Dewey WL, Selley DE, Zhang Y.
J Med Chem (2023) 66 : 577 -595
PubMed 36538027 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 35 9.09 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5399596 1 9.64
CHEMBL4595328 1 9.64
CHEMBL5423403 1 9.60
CHEMBL5427274 1 9.57
CHEMBL5432174 1 9.51
CHEMBL5417637 1 9.46
CHEMBL5416619 1 9.42
CHEMBL5432205 1 9.37
CHEMBL5432317 1 9.34
CHEMBL5426766 1 9.32
CHEMBL5420457 1 9.27
CHEMBL5432371 1 9.23
CHEMBL5440937 1 9.21
CHEMBL5431128 1 9.20
CHEMBL5415668 1 9.19
CHEMBL5434721 1 9.16
CHEMBL5411900 1 9.16
CHEMBL5401578 1 9.15
CHEMBL5438077 1 9.14
CHEMBL5427896 1 9.06
CHEMBL5425838 1 9.06
CHEMBL5405519 1 9.05
CHEMBL5405800 1 9.03
CHEMBL5425108 1 9.01
CHEMBL5417814 1 8.97
CHEMBL5434911 1 8.84
CHEMBL5398970 1 8.84
CHEMBL5396504 1 8.68
CHEMBL5429587 1 8.62
CHEMBL5424438 1 8.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5399596 Ki = 0.23 nM 9.64
CHEMBL4595328 Ki = 0.23 nM 9.64
CHEMBL5423403 Ki = 0.25 nM 9.60
CHEMBL5427274 Ki = 0.27 nM 9.57
CHEMBL5432174 Ki = 0.31 nM 9.51
CHEMBL5417637 Ki = 0.35 nM 9.46
CHEMBL5416619 Ki = 0.38 nM 9.42
CHEMBL5432205 Ki = 0.43 nM 9.37
CHEMBL5432317 Ki = 0.46 nM 9.34
CHEMBL5426766 Ki = 0.48 nM 9.32
CHEMBL5420457 Ki = 0.54 nM 9.27
CHEMBL5432371 Ki = 0.59 nM 9.23
CHEMBL5440937 Ki = 0.62 nM 9.21
CHEMBL5431128 Ki = 0.63 nM 9.20
CHEMBL5415668 Ki = 0.65 nM 9.19
CHEMBL5434721 Ki = 0.69 nM 9.16
CHEMBL5411900 Ki = 0.69 nM 9.16
CHEMBL5401578 Ki = 0.7 nM 9.15
CHEMBL5438077 Ki = 0.73 nM 9.14
CHEMBL5427896 Ki = 0.87 nM 9.06
CHEMBL5425838 Ki = 0.87 nM 9.06
CHEMBL5405519 Ki = 0.89 nM 9.05
CHEMBL5405800 Ki = 0.93 nM 9.03
CHEMBL5425108 Ki = 0.98 nM 9.01
CHEMBL5417814 Ki = 1.07 nM 8.97
CHEMBL5398970 Ki = 1.45 nM 8.84
CHEMBL5434911 Ki = 1.46 nM 8.84
CHEMBL5396504 Ki = 2.11 nM 8.68
CHEMBL5429587 Ki = 2.37 nM 8.62
CHEMBL5424438 Ki = 2.45 nM 8.61
CHEMBL5424642 Ki = 2.66 nM 8.57
CHEMBL5403273 Ki = 2.78 nM 8.56
CHEMBL5419838 Ki = 3.26 nM 8.49
CHEMBL5406491 Ki = 5.57 nM 8.25
CHEMBL5434134 Ki > 50.0 nM -