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Assay Detail

CHEMBL2168755

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

Binding
Displacement of [125I]-dY-peptide from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by by liquid scintillation counting
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Bombesin receptor subtype-3 (CHEMBL4080)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of MK-7725, A Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
Chobanian HR, Guo Y, Liu P, Chioda M, Lanza TJ, Chang L, Kelly TM, Kan Y, Palyha O, Guan XM, Marsh DJ, Metzger JM, Gorski JN, Raustad K, Wang SP, Strack AM, Miller R, Pang J, Madeira M, Lyons K, Dragovic J, Reitman ML, Nargund RP, Lin LS.
ACS Med Chem Lett (2012) 3 : 252 -256
PubMed 24900461 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 8.62 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2164581 1 9.15
CHEMBL2164577 1 9.12
CHEMBL2164223 1 9.05
CHEMBL2164580 1 8.96
CHEMBL2164582 1 8.92
CHEMBL2164578 1 8.85
CHEMBL2164224 1 8.77
CHEMBL2164576 1 8.76
CHEMBL2164222 1 8.72
CHEMBL2023109 1 8.44
CHEMBL2164225 1 8.08
CHEMBL2164226 1 7.75
CHEMBL2164579 1 7.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2164581 IC50 = 0.7 nM 9.15
CHEMBL2164577 IC50 = 0.76 nM 9.12
CHEMBL2164223 IC50 = 0.9 nM 9.05
CHEMBL2164580 IC50 = 1.1 nM 8.96
CHEMBL2164582 IC50 = 1.2 nM 8.92
CHEMBL2164578 IC50 = 1.4 nM 8.85
CHEMBL2164224 IC50 = 1.7 nM 8.77
CHEMBL2164576 IC50 = 1.72 nM 8.76
CHEMBL2164222 IC50 = 1.9 nM 8.72
CHEMBL2023109 IC50 = 3.6 nM 8.44
CHEMBL2164225 IC50 = 8.3 nM 8.08
CHEMBL2164226 IC50 = 18.0 nM 7.75
CHEMBL2164579 IC50 = 29.0 nM 7.54