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Assay Detail

CHEMBL854079

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

Binding
Binding affinity at the CB1 receptor
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Cannabinoid receptor 1 (CHEMBL218)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists.
Debenham JS, Madsen-Duggan CB, Walsh TF, Wang J, Tong X, Doss GA, Lao J, Fong TM, Schaeffer MT, Xiao JC, Huang CR, Shen CP, Feng Y, Marsh DJ, Stribling DS, Shearman LP, Strack AM, MacIntyre DE, Van der Ploeg LH, Goulet MT.
Bioorg Med Chem Lett (2006) 16 : 681 -685
PubMed 16263284 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.67 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL201388 1 8.64
CHEMBL202169 1 8.64
CHEMBL371252 1 8.43
CHEMBL202064 1 8.28
CHEMBL204232 NAPHTHYRIDINONE 1 8.12
CHEMBL381677 1 7.82
CHEMBL202659 1 7.70
CHEMBL201102 1 7.62
CHEMBL201552 1 7.62
CHEMBL202013 1 7.58
CHEMBL380483 1 7.50
CHEMBL265787 1 7.46
CHEMBL202201 1 7.34
CHEMBL202202 1 7.26
CHEMBL203152 1 7.11
CHEMBL370388 1 7.02
CHEMBL204391 1 6.96
CHEMBL203811 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL201388 IC50 = 2.3 nM 8.64
CHEMBL202169 IC50 = 2.3 nM 8.64
CHEMBL371252 IC50 = 3.7 nM 8.43
CHEMBL202064 IC50 = 5.2 nM 8.28
CHEMBL204232 NAPHTHYRIDINONE IC50 = 7.5 nM 8.12
CHEMBL381677 IC50 = 15.0 nM 7.82
CHEMBL202659 IC50 = 20.0 nM 7.70
CHEMBL201102 IC50 = 24.0 nM 7.62
CHEMBL201552 IC50 = 24.0 nM 7.62
CHEMBL202013 IC50 = 26.0 nM 7.58
CHEMBL380483 IC50 = 32.0 nM 7.50
CHEMBL265787 IC50 = 35.0 nM 7.46
CHEMBL202201 IC50 = 46.0 nM 7.34
CHEMBL202202 IC50 = 55.0 nM 7.26
CHEMBL203152 IC50 = 77.0 nM 7.11
CHEMBL370388 IC50 = 96.0 nM 7.02
CHEMBL204391 IC50 = 110.0 nM 6.96
CHEMBL203811 IC50 = 120.0 nM 6.92