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Assay Detail

CHEMBL1680282

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Functional
Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay
8
Total Activities
8
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-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
EC50 8 7.20 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1671874 1 7.85
CHEMBL1672354 1 7.85
CHEMBL1672353 1 7.80
CHEMBL1091720 1 7.33
CHEMBL1093184 1 7.18
CHEMBL1672352 1 7.17
CHEMBL1672351 1 6.66
CHEMBL1079517 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1671874 EC50 = 14.0 nM 7.85
CHEMBL1672354 EC50 = 14.0 nM 7.85
CHEMBL1672353 EC50 = 16.0 nM 7.80
CHEMBL1091720 EC50 = 47.0 nM 7.33
CHEMBL1093184 EC50 = 66.0 nM 7.18
CHEMBL1672352 EC50 = 67.0 nM 7.17
CHEMBL1672351 EC50 = 220.0 nM 6.66
CHEMBL1079517 EC50 = 1900.0 nM 5.72