Bombesin BDBM85484
Bombesin,Phe13 BDBM85500
BDBM50089292 CHEMBL439440 Bombesin analogues
BDBM50089293 Bombesin analogues CHEMBL407481
BDBM50158701 [Tyr4]Bombesin CHEMBL407101
Bombesin analogue CHEMBL269432 BDBM50288252
Bombesin analogues BDBM50089289 CHEMBL384241
Bombesin analogues CHEMBL384242 BDBM50089287
CHEMBL413938 BDBM50089290 Bombesin analogues
CHEMBL415022 Bombesin analogues BDBM50089288
CAS_31362-50-2 Bombesin, SAP BDBM85478
CHEMBL262992 [D-Tyr6-, Beta-Ala11, Phe13, Nle14] Bn (6-14)(Bombesin Analogue) BDBM50127519
Bombesin CAS_5490336 Pyr-Gln-Arg-Leu-Gly-Asn-Gln-Trp-Ala-Val-Gly-His-Leu-Met-NH2 BDBM86499
- Cristau, M; Devin, C; Oiry, C; Chaloin, O; Amblard, M; Bernad, N; Heitz, A; Fehrentz, JA; Martinez, J Synthesis and biological evaluation of bombesin constrained analogues. J Med Chem 43: 2356-61 (2000)
- Mantey, SA; Coy, DH; Entsuah, LK; Jensen, RT Development of bombesin analogs with conformationally restricted amino acid substitutions with enhanced selectivity for the orphan receptor human bombesin receptor subtype 3. J Pharmacol Exp Ther 310: 1161-70 (2004)
- Gourni, E; Bouziotis, P; Benaki, D; Loudos, G; Xanthopoulos, S; Paravatou-Petsotas, M; Mavri-Vavagianni, M; Pelecanou, M; Archimandritis, SC; Varvarigou, AD Structural assessment and biological evaluation of two N3S bombesin derivatives. J Med Chem 52: 4234-46 (2009)
- Katsuno, T; Pradhan, TK; Ryan, RR; Mantey, SA; Hou, W; Donohue, PJ; Akeson, MA; Spindel, ER; Battey, JF; Coy, DH; Jensen, RT Pharmacology and cell biology of the bombesin receptor subtype 4 (BB4-R). Biochemistry 38: 7307-20 (1999)
- Lo, MM; Chobanian, HR; Palyha, O; Kan, Y; Kelly, TM; Guan, XM; Reitman, ML; Dragovic, J; Lyons, KA; Nargund, RP; Lin, LS Pyridinesulfonylureas and pyridinesulfonamides as selective bombesin receptor subtype-3 (BRS-3) agonists. Bioorg Med Chem Lett 21: 2040-3 (2011)
- Pourghiasian, M; Liu, Z; Pan, J; Zhang, Z; Colpo, N; Lin, KS; Perrin, DM; Bénard, F (18)F-AmBF3-MJ9: a novel radiofluorinated bombesin derivative for prostate cancer imaging. Bioorg Med Chem 23: 1500-6 (2015)
- He, S; Dobbelaar, PH; Liu, J; Jian, T; Sebhat, IK; Lin, LS; Goodman, A; Guo, C; Guzzo, PR; Hadden, M; Henderson, AJ; Ruenz, M; Sargent, BJ; Yet, L; Kelly, TM; Palyha, O; Kan, Y; Pan, J; Chen, H; Marsh, DJ; Shearman, LP; Strack, AM; Metzger, JM; Feighner, SD; Tan, C; Howard, AD; Tamvakopoulos, C; Peng, Q; Guan, XM; Reitman, ML; Patchett, AA; Wyvratt, MJ; Nargund, RP Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists. Bioorg Med Chem Lett 20: 1913-7 (2010)
- Axarli, I; Labrou, NE; Petrou, C; Rassias, N; Cordopatis, P; Clonis, YD Sulphonamide-based bombesin prodrug analogues for glutathione transferase, useful in targeted cancer chemotherapy. Eur J Med Chem 44: 2009-16 (2009)
- Liu, P; Lanza, TJ; Chioda, M; Jones, C; Chobanian, HR; Guo, Y; Chang, L; Kelly, TM; Kan, Y; Palyha, O; Guan, XM; Marsh, DJ; Metzger, JM; Ramsay, K; Wang, SP; Strack, AM; Miller, R; Pang, J; Lyons, K; Dragovic, J; Ning, JG; Schafer, WA; Welch, CJ; Gong, X; Gao, YD; Hornak, V; Ball, RG; Tsou, N; Reitman, ML; Wyvratt, MJ; Nargund, RP; Lin, LS Discovery of benzodiazepine sulfonamide-based bombesin receptor subtype 3 agonists and their unusual chirality. ACS Med Chem Lett 2: 933-937 (2011)
- Nock, BA; Nikolopoulou, A; Galanis, A; Cordopatis, P; Waser, B; Reubi, JC; Maina, T Potent bombesin-like peptides for GRP-receptor targeting of tumors with 99mTc: a preclinical study. J Med Chem 48: 100-10 (2005)
- Valentine, JJ; Nakanishi, S; Hageman, DL; Snider, R; Spencer, RW; Vinick, FJ CP-70,030 and CP-75,998: The first non-peptide antagonists of bombesin and gastrin releasing peptide Bioorg Med Chem Lett 2: 333-338 (1992)
- 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 Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity ACS Med Chem Lett 2: 43-47 (2011)
- 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 Discovery of MK-7725, A Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity. ACS Med Chem Lett 3: 252-256 (2012)
- Matsufuji, T; Shimada, K; Kobayashi, S; Kawamura, A; Fujimoto, T; Arita, T; Hara, T; Konishi, M; Abe-Ohya, R; Izumi, M; Sogawa, Y; Nagai, Y; Yoshida, K; Takahashi, H Discovery of novel chiral diazepines as bombesin receptor subtype-3 (BRS-3) agonists with low brain penetration. Bioorg Med Chem Lett 24: 750-5 (2014)
- Dubuc, C; Langlois, R; Bénard, F; Cauchon, N; Klarskov, K; Tone, P; van Lier, JE Targeting gastrin-releasing peptide receptors of prostate cancer cells for photodynamic therapy with a phthalocyanine-bombesin conjugate. Bioorg Med Chem Lett 18: 2424-7 (2008)
- Carlton, DL; Collin-Smith, LJ; Daniels, AJ; Deaton, DN; Goetz, AS; Laudeman, CP; Littleton, TR; Musso, DL; Morgan, RJ; Szewczyk, JR; Zhang, C Discovery of small molecule agonists for the bombesin receptor subtype 3 (BRS-3) based on an omeprazole lead. Bioorg Med Chem Lett 18: 5451-5 (2008)
- Matsufuji, T; Shimada, K; Kobayashi, S; Ichikawa, M; Kawamura, A; Fujimoto, T; Arita, T; Hara, T; Konishi, M; Abe-Ohya, R; Izumi, M; Sogawa, Y; Nagai, Y; Yoshida, K; Abe, Y; Kimura, T; Takahashi, H Synthesis and biological evaluation of novel chiral diazepine derivatives as bombesin receptor subtype-3 (BRS-3) agonists incorporating an antedrug approach. Bioorg Med Chem 23: 89-104 (2014)
- Liu, J; He, S; Jian, T; Dobbelaar, PH; Sebhat, IK; Lin, LS; Goodman, A; Guo, C; Guzzo, PR; Hadden, M; Henderson, AJ; Pattamana, K; Ruenz, M; Sargent, BJ; Swenson, B; Yet, L; Tamvakopoulos, C; Peng, Q; Pan, J; Kan, Y; Palyha, O; Kelly, TM; Guan, XM; Howard, AD; Marsh, DJ; Metzger, JM; Reitman, ML; Wyvratt, MJ; Nargund, RP Synthesis and SAR of derivatives based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity. Bioorg Med Chem Lett 20: 2074-7 (2010)
- Kiyotsuka, Y; Shimada, K; Kobayashi, S; Suzuki, M; Akiu, M; Asano, M; Sogawa, Y; Hara, T; Konishi, M; Abe-Ohya, R; Izumi, M; Nagai, Y; Yoshida, K; Abe, Y; Takamori, H; Takahashi, H Synthesis and biological evaluation of novel imidazol-1-ylacetic acid derivatives as non-brain penetrant bombesin receptor subtype-3 (BRS-3) agonists. Bioorg Med Chem Lett 26: 4205-10 (2016)
- Chobanian, HR; Guo, Y; Liu, P; Lanza, TJ; Chioda, M; Chang, L; Kelly, TM; Kan, Y; Palyha, O; Guan, XM; Marsh, DJ; Metzger, JM; Raustad, K; Wang, SP; Strack, AM; Gorski, JN; Miller, R; Pang, J; Lyons, K; Dragovic, J; Ning, JG; Schafer, WA; Welch, CJ; Gong, X; Gao, YD; Hornak, V; Reitman, ML; Nargund, RP; Lin, LS The design and synthesis of potent, selective benzodiazepine sulfonamide bombesin receptor subtype 3 (BRS-3) agonists with an increased barrier of atropisomerization. Bioorg Med Chem 20: 2845-9 (2012)
- Liu, Z; Yan, Y; Chin, FT; Wang, F; Chen, X Dual integrin and gastrin-releasing peptide receptor targeted tumor imaging using 18F-labeled PEGylated RGD-bombesin heterodimer 18F-FB-PEG3-Glu-RGD-BBN. J Med Chem 52: 425-32 (2009)
- Hadden, M; Goodman, A; Guo, C; Guzzo, PR; Henderson, AJ; Pattamana, K; Ruenz, M; Sargent, BJ; Swenson, B; Yet, L; Liu, J; He, S; Sebhat, IK; Lin, LS; Tamvakopoulos, C; Peng, Q; Kan, Y; Palyha, O; Kelly, TM; Guan, XM; Metzger, JM; Reitman, ML; Nargund, RP Synthesis and SAR of heterocyclic carboxylic acid isosteres based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity. Bioorg Med Chem Lett 20: 2912-5 (2010)
- Guo, C; Guzzo, PR; Hadden, M; Sargent, BJ; Yet, L; Kan, Y; Palyha, O; Kelly, TM; Guan, X; Rosko, K; Gagen, K; Metzger, JM; Dragovic, J; Lyons, K; Lin, LS; Nargund, RP Synthesis of 7-benzyl-5-(piperidin-1-yl)-6,7,8,9-tetrahydro-3H-pyrazolo[3,4-c][2,7]naphthyridin-1-ylamine and its analogs as bombesin receptor subtype-3 agonists. Bioorg Med Chem Lett 20: 2785-9 (2010)
- ChEBML_39763 In vitro binding affinity at Bombesin BB2 receptor in the presence of [125I]-[Tyr] bombesin.
- ChEBML_39622 Antagonistic activity against labelled Bombesin receptor bb1 binding sites in rat olfactory bulb by using [125I]- [Tyr] bombesin in presence of [D-Phe-6] bombesin(6-13)ethyl ester; 0.31-1.3
- ChEMBL_39622 (CHEMBL649929) Antagonistic activity against labelled Bombesin receptor bb1 binding sites in rat olfactory bulb by using [125I]- [Tyr] bombesin in presence of [D-Phe-6] bombesin(6-13)ethyl ester; 0.31-1.3
- ChEMBL_39620 (CHEMBL649928) In vitro binding affinity of [111In]DTPA-[Y4]-bombesin to bombesin receptor in the rat pancreatic acinar cell line, AR42J
- ChEMBL_39764 (CHEMBL650354) Antagonistic activity against cloned human Bombesin receptor bb2 labeled with [125I]- [Tyr] bombesin stably expressed in CHO cells; 0.66-1.3
- ChEMBL_39762 (CHEMBL883283) Antagonistic activity against labelled Bombesin receptor bb2 binding sites in rat cerebral cortex by using [125I]- [Tyr] bombesin in presence of NMB; 6.5-31
- ChEMBL_614942 (CHEMBL1115979) Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]bombesin from human bombesin BB1 receptor expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting
- ChEMBL_614943 (CHEMBL1115980) Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]bombesin from human bombesin BB2 receptor expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting
- ChEMBL_306145 (CHEMBL831380) Inhibition of bombesin subtype 3 receptor expressed in human lung carcinoids
- ChEMBL_39236 (CHEMBL655732) In vitro binding affinity against bombesin / GRP receptors on rat pancreatic acini.
- ChEMBL_470060 (CHEMBL933438) Displacement of 125I[Tyr4]-bombesin from GRPR expressed in human PC3 cells
- ChEMBL_985515 (CHEMBL2432761) Displacement of [125I]-Tyr4-bombesin from GRP receptor in human PC3 cells
- ChEBML_143209 Binding affinity against NMB receptor in rat olfactory bulb was determined using [125I]-[Tyr4] bombesin.
- ChEMBL_718486 (CHEMBL1680281) Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3
- ChEMBL_39239 (CHEMBL655889) Effective concentration required against human bombesin receptor 3 (BRS-3) in CHO cells by using FLIPR assay.
- ChEBML_71531 Binding affinity against [125 I][4Tyr]-bombesin labeled cloned human GRP(gastrin releasing peptide) receptors stably expressed in CHO cells
- ChEMBL_740056 (CHEMBL1763116) Displacement of [125I]-[D-Tyr6, b-Ala11, Phe13, Nle14]-Bombesin (6-14) from human BRS3 by competitive binding assay
- ChEMBL_985653 (CHEMBL2433419) Displacement of [125I]-Tyr4-bombesin from GRP receptor in human PC3 cells after 1 hr by gamma-counting analysis
- ChEMBL_1464741 (CHEMBL3407092) Displacement of [125I-Tyr4]bombesin from GRPR (unknown origin) expressed in human PC3 cells after 45 mins by gamma counting analysis
- ChEMBL_627760 (CHEMBL1116182) Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
- ChEMBL_627765 (CHEMBL1116187) Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human NMB-R expressed in NFAT-CHO cells after 2 hrs by scintillation counting
- ChEMBL_627766 (CHEMBL1116188) Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human GRP-R expressed in NFAT-CHO cells after 2 hrs by scintillation counting
- ChEMBL_627767 (CHEMBL1116189) Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from rat BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
- ChEMBL_627768 (CHEMBL1116190) Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from mouse BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting
- ChEMBL_614786 (CHEMBL1113305) Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]bombesin from human BRS3 expressed in NFAT-CHO cells after 2 hrs by liquid scintillation counting
- ChEMBL_627762 (CHEMBL1116184) Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
- ChEMBL_627764 (CHEMBL1116186) Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin
- ChEMBL_872481 (CHEMBL2182521) Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin(6-14) from human BRS3 expressed in CHO cells expressing NFAT after 2 hrs by liquid scintillation counting
- BB2 Receptor Antagonistic Activity A BB2 receptor binding test was carried out using a membrane sample prepared from a human prostate cancer-derived PC-3 cell. The PC-3 cell was cultured using an RPMI-1640 medium containing 5% fetal bovine serum, and then a membrane sample was prepared by the following methods. The cells detached by a trypsin treatment were added with a 50 mM Tris-HCl buffer (pH 7.4, containing 0.2 mg/ml trypsin inhibitor and 0.2 mg/ml benzamidine), and homogenized by Polytron. The cell suspension was centrifuged at 1,500 rpm for 10 minutes, and the supernatant thus obtained was subjected to 1 hour of ultracentrifugation at 37,000×g. The precipitate was suspended in the aforementioned buffer to a concentration of 0.4 mg protein/ml, and stored at −80° C.The BB2 receptor binding test was carried out by the following method, and the receptor antagonistic activity of a compound to be tested was calculated. A 50 μl of the membrane sample, 50 μl of an assay buffer (20 mM HEPES-HBSS containing 0.1% bovine serum albumin and 0.1 mg/ml bacitracin, pH 7.4), 125I [Tyr4] bombesin (0.075 nM) and 2 μl of the compound to be tested dissolved in dimethyl sulfoxide were added to a 96 well assay plate, and incubated at room temperature for 2 hours. Non-specific binding was measured using 1 μM of bombesin. After completion of the incubation, the reaction solution was filtered through a Whatman GF/B filter which had been soaked in 0.5% polyethyleneimine. The radioactivity on the filter was measured using a microplate scintillation counter (Top Count, Perkin-Elmer Co., Ltd.).