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Assay Detail

CHEMBL1680281

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

Binding
Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
7
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
Sebhat IK, Franklin C, Lo MM, Chen D, Jewell JP, Miller R, Pang J, Palyha O, Kan Y, Kelly TM, Guan XM, Marsh DJ, Kosinski JA, Metzger JM, Lyons K, Dragovic J, Guzzo PR, Henderson AJ, Reitman ML, Nargund RP, Wyvratt MJ, Lin LS.
ACS Med Chem Lett (2011) 2 : 43 -47
PubMed 24900253 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.75 8.30
Ki 1 8.43 8.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1672354 2 8.43
CHEMBL1672353 1 8.30
CHEMBL1671874 1 7.96
CHEMBL1093184 1 7.80
CHEMBL1672352 1 7.77
CHEMBL1672351 1 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1672354 Ki = 3.7 nM 8.43
CHEMBL1672353 IC50 = 5.0 nM 8.30
CHEMBL1671874 IC50 = 11.0 nM 7.96
CHEMBL1093184 IC50 = 16.0 nM 7.80
CHEMBL1672352 IC50 = 17.0 nM 7.77
CHEMBL1672354 IC50 = 27.0 nM 7.57
CHEMBL1672351 IC50 = 82.0 nM 7.09