mk 5046 profile

ID Source	ID
PubMed CID	49871766
CHEMBL ID	1672354
SCHEMBL ID	3499662
MeSH ID	M0555207

Synonym
CHEMBL1672354 ,
mk-5046
bdbm50336889
(2s)-1,1,1-trifluoro-2-[4-(1h-pyrazol-1-yl)phenyl]-3-(4-{[1-(trifluoromethyl)cyclopropyl]methyl}-1h-imidazol-2-yl)propan-2-ol
mk5046
(2s)-1,1,1-trifluoro-2-(4-pyrazol-1-ylphenyl)-3-[5-[[1-(trifluoromethyl)cyclopropyl]methyl]-1h-imidazol-2-yl]propan-2-ol
mk 5046
gtpl6170
SCHEMBL3499662
CS-4808
HY-14342
mk5046 peak 2
1022152-70-0
(s)-2-(4-(1h-pyrazol-1-yl)phenyl)-1,1,1-trifluoro-3-(5-((1-(trifluoromethyl)cyclopropyl)methyl)-1h-imidazol-2-yl)propan-2-ol
NCGC00484084-01
1h-imidazole-2-ethanol, a-[4-(1h-pyrazol-1-yl)phenyl]-a-(trifluoromethyl)-5-[[1-(trifluoromethyl)cyclopropyl]methyl]-, (as)-;1h-imidazole-2-ethanol, a-[4-(1h-pyrazol-1-yl)phenyl]-a-(trifluoromethyl)-5-[[1-(trifluoromethyl)cyclopropyl]methyl]-, (as)-
AKOS032960467
BCP23816
mk-5046; mk 5046
1022152-69-7
mk5046 peak 1
Q27086837
EX-A2796
MS-28002
ujinbeqcdmoahm-sfhvurjksa-n
unii-qhz72h8f6p
(2s)-1,1,1-trifluoro-2-(4-(1h-pyrazol-1-yl)phenyl)-3-(4-((1-(trifluoromethyl)cyclopropyl)methyl)-1h-imidazol-2-yl)propan-2-ol
qhz72h8f6p ,
1h-imidazole-2-ethanol, alpha-(4-(1h-pyrazol-1-yl)phenyl)-alpha-(trifluoromethyl)-5-((1-(trifluoromethyl)cyclopropyl)methyl)-, (alphas)-
1h-imidazole-2-ethanol, alpha-[4-(1h-pyrazol-1-yl)phenyl]-alpha-(trifluoromethyl)-5-[[1-(trifluoromethyl)cyclopropyl]methyl]-, (alphas)-

Excerpt	Reference	Relevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51

Excerpt	Relevance	Reference
" Upon dosing for 14 days, MK-5046 at 25 mg · kg(-1) · day(-1) reduced body weight of diet-induced obese mouse by 9% compared with vehicle-dosed controls."	( Antiobesity effect of MK-5046, a novel bombesin receptor subtype-3 agonist. Craw, S; Dragovic, J; Faidley, TD; Guan, XM; Kan, Y; Kelly, TM; Kosinski, JA; Lin, LS; Lyons, KA; Marsh, DJ; Metzger, JM; Nargund, RP; Palyha, O; Raustad, KA; Reitman, ML; Sebhat, I; Shearman, LP; Spann, SK; Strack, AM; Wang, SP; Yang, L; Yu, H, 2011)	0.37

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Bombesin receptor subtype-3	Mus musculus (house mouse)	IC50 (µMol)	0.0054	0.0054	0.0054	0.0054	AID569962
Bombesin receptor subtype-3	Mus musculus (house mouse)	Ki	0.0016	0.0016	0.0016	0.0016	AID569962
Bombesin receptor subtype-3	Homo sapiens (human)	IC50 (µMol)	0.0270	0.0270	0.0270	0.0270	AID569946
Bombesin receptor subtype-3	Homo sapiens (human)	Ki	0.0037	0.0037	0.0037	0.0037	AID569946
Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)	Ki	8.0000	0.0021	1.8407	10.0000	AID569954
Bombesin receptor subtype-3	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.0012	0.0012	0.0012	0.0012	AID569963
Bombesin receptor subtype-3	Rattus norvegicus (Norway rat)	Ki	0.0006	0.0006	0.0006	0.0006	AID569963
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Bombesin receptor subtype-3	Mus musculus (house mouse)	EC50 (µMol)	0.0210	0.0210	0.0210	0.0210	AID1176122; AID570337
Metabotropic glutamate receptor 5	Rattus norvegicus (Norway rat)	EC50 (µMol)	0.0140	0.0015	1.6537	10.0000	AID569947
Bombesin receptor subtype-3	Homo sapiens (human)	EC50 (µMol)	0.0140	0.0140	1.3093	3.9000	AID1176121; AID569947
Bombesin receptor subtype-3	Rattus norvegicus (Norway rat)	EC50 (µMol)	0.0022	0.0022	0.0022	0.0022	AID570339
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
glucose metabolic process	Bombesin receptor subtype-3	Homo sapiens (human)
neuropeptide signaling pathway	Bombesin receptor subtype-3	Homo sapiens (human)
regulation of blood pressure	Bombesin receptor subtype-3	Homo sapiens (human)
adult feeding behavior	Bombesin receptor subtype-3	Homo sapiens (human)
bombesin receptor signaling pathway	Bombesin receptor subtype-3	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Bombesin receptor subtype-3	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate by hormone	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of membrane potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
positive regulation of DNA-templated transcription	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion homeostasis	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cardiac muscle contraction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cellular response to xenobiotic stimulus	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane depolarization during action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
negative regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
positive regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
negative regulation of potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion import across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
bombesin receptor activity	Bombesin receptor subtype-3	Homo sapiens (human)
neuropeptide receptor activity	Bombesin receptor subtype-3	Homo sapiens (human)
transcription cis-regulatory region binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
delayed rectifier potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
ubiquitin protein ligase binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
identical protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein homodimerization activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
C3HC4-type RING finger domain binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
scaffold protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
membrane	Bombesin receptor subtype-3	Homo sapiens (human)
plasma membrane	Bombesin receptor subtype-3	Homo sapiens (human)
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cell surface	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
perinuclear region of cytoplasm	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (58)

Assay ID	Title	Year	Journal	Article
AID570360	Plasma clearance in rhesus monkey at 0.5 mg/kg, iv	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID569954	Binding affinity to human ERG	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570354	Oral bioavailability in rat at 2 mg/kg	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID569962	Displacement of [3H]Bag-3 from mouse BRS-3	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID569948	Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay relative to dY peptide	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570344	Agonist activity at rhesus monkey BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay relative to dY peptide	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570335	Binding affinity to dog BRS-3	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID569946	Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570338	Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay relative to control	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570341	Agonist activity at dog BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID1176121	Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay	2015	Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1	Synthesis and biological evaluation of novel chiral diazepine derivatives as bombesin receptor subtype-3 (BRS-3) agonists incorporating an antedrug approach.
AID570364	Antiobesity activity in wild type mouse assessed as increase of fasting metabolic rate	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570340	Agonist activity at rat BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay relative to control	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570359	Oral bioavailability in rhesus monkey at 1 mg/kg	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID569961	Oral bioavailability in dog at 1 mg/kg	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570349	Oral bioavailability in mouse at 2 mg/kg, po	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570336	Binding affinity to rhesus monkey BRS-3	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID569963	Displacement of [3H]Bag-3 from rat BRS-3	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID569947	Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID569957	Fraction unbound in rat plasma at 1 uM	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570350	Plasma clearance in mouse at 1 mg/kg, iv	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570337	Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570356	Half life in rat at 1 mg/kg, iv	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570368	Antiobesity activity in eDIO mouse assessed as reduction of body weight at 25 mg/kg, sc after 14 days	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570353	Normalized AUC in rat at 2 mg/kg, po	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570367	Antiobesity activity in eDIO mouse assessed as reduction of body weight at 25 mg/kg, sc relative to control	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570348	Normalized AUC in mouse at 2 mg/kg, po	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570342	Agonist activity at dog BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay relative to dY peptide	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570352	Half life in mouse at 1 mg/kg, iv	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570361	Volume of distribution at steady state in rhesus monkey at 0.5 mg/kg, iv	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID569949	Half life in rat liver microsomes	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID1176122	Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay	2015	Bioorganic & medicinal chemistry, Jan-01, Volume: 23, Issue:1	Synthesis and biological evaluation of novel chiral diazepine derivatives as bombesin receptor subtype-3 (BRS-3) agonists incorporating an antedrug approach.
AID569955	Plasma clearance in rat at 1 mg/kg, iv	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID569956	Faction unbound in human plasma at 1 uM	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570343	Agonist activity at rhesus monkey BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570363	Antiobesity activity in wild type mouse assessed as reduction of food intake	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570355	Volume of distribution at steady state in rat at 1 mg/kg, iv	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570362	Half life in rhesus monkey at 0.5 mg/kg, iv	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570366	Antiobesity activity in BRS3 deficient mouse assessed as increase of fasting metabolic rate	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570351	Volume of distribution at steady state in mouse at 1 mg/kg, iv	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570365	Antiobesity activity in BRS3 deficient mouse assessed as reduction of food intake	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID569959	Half life in dog at 0.5 mg/kg, iv	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570357	Volume of distribution at steady state in dog at 0.5 mg/kg, iv	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID569960	Normalized AUC in dog at 1 mg/kg, po	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570358	Normalized AUC in rhesus monkey at 1 mg/kg, po	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID570339	Agonist activity at rat BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID569958	Plasma clearance in dog at 0.5 mg/kg, iv	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347160	Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346539	Human BB2 receptor (Bombesin receptors)	2013	The Journal of pharmacology and experimental therapeutics, Oct, Volume: 347, Issue:1	Comparative pharmacology of bombesin receptor subtype-3, nonpeptide agonist MK-5046, a universal peptide agonist, and peptide antagonist Bantag-1 for human bombesin receptors.
AID1346439	Human BB1 receptor (Bombesin receptors)	2011	The Journal of pharmacology and experimental therapeutics, Feb, Volume: 336, Issue:2	Antiobesity effect of MK-5046, a novel bombesin receptor subtype-3 agonist.
AID1346494	Human BB3 receptor (Class A Orphans)	2011	ACS medicinal chemistry letters, Jan-13, Volume: 2, Issue:1	Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
AID1346439	Human BB1 receptor (Bombesin receptors)	2013	The Journal of pharmacology and experimental therapeutics, Oct, Volume: 347, Issue:1	Comparative pharmacology of bombesin receptor subtype-3, nonpeptide agonist MK-5046, a universal peptide agonist, and peptide antagonist Bantag-1 for human bombesin receptors.
AID1346499	Mouse BB3 receptor (Class A Orphans)	2011	The Journal of pharmacology and experimental therapeutics, Feb, Volume: 336, Issue:2	Antiobesity effect of MK-5046, a novel bombesin receptor subtype-3 agonist.
AID1346494	Human BB3 receptor (Class A Orphans)	2013	The Journal of pharmacology and experimental therapeutics, Oct, Volume: 347, Issue:1	Comparative pharmacology of bombesin receptor subtype-3, nonpeptide agonist MK-5046, a universal peptide agonist, and peptide antagonist Bantag-1 for human bombesin receptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	5 (71.43)	24.3611
2020's	2 (28.57)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	7 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Condition	Relationship Strength	Studies
Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.	2.06	1
Obesity A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).	2.11	1
Congenital Zika Syndrome [description not available]	2.25	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.25	1
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	2.25	1

mk 5046

Cross-References

Synonyms (30)

Research Excerpts

Bioavailability

Dosage Studied

Protein Targets (5)

Inhibition Measurements

Activation Measurements

Biological Processes (28)

Molecular Functions (14)

Ceullar Components (6)

Bioassays (58)

Research

Studies (7)

Market Indicators

Research Demand Index: 28.12

Study Types

mk 5046

Cross-References

Synonyms (30)

Research Excerpts

Bioavailability

Dosage Studied

Protein Targets (5)

Inhibition Measurements

Activation Measurements

Biological Processes (28)

Molecular Functions (14)

Ceullar Components (6)

Bioassays (58)

Research

Studies (7)

Market Indicators

Research Demand Index: 28.12

Study Types

Related Conditions (5)