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Assay Detail

CHEMBL2168754

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

Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as bioluminescence for 10 mins by aequorin bioluminescence assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
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
EC50 9 7.22 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2164580 1 7.40
CHEMBL2164576 1 7.38
CHEMBL2164223 1 7.28
CHEMBL2164582 1 7.28
CHEMBL2164581 1 7.25
CHEMBL2164577 1 7.20
CHEMBL2164222 1 7.16
CHEMBL2164579 1 7.11
CHEMBL2164578 1 6.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2164580 EC50 = 40.0 nM 7.40
CHEMBL2164576 EC50 = 42.0 nM 7.38
CHEMBL2164223 EC50 = 52.0 nM 7.28
CHEMBL2164582 EC50 = 52.0 nM 7.28
CHEMBL2164581 EC50 = 56.0 nM 7.25
CHEMBL2164577 EC50 = 63.0 nM 7.20
CHEMBL2164222 EC50 = 69.0 nM 7.16
CHEMBL2164579 EC50 = 77.0 nM 7.11
CHEMBL2164578 EC50 = 114.0 nM 6.94