ChEMBL ligand: CHEMBL1672354 (MK-5046)
BB3 receptor/Bombesin receptor subtype-3 in Human [ChEMBL: CHEMBL4080] [GtoPdb: 40] [UniProtKB: P32247] BB3 receptor/Bombesin receptor subtype-3 in Mouse [ChEMBL: CHEMBL1075140] [GtoPdb: 40] [UniProtKB: O54798] BB3 receptor/Bombesin receptor subtype-3 in Rat [ChEMBL: CHEMBL1075111] [GtoPdb: 40] [UniProtKB: Q8K418] There should be some charts here, you may need to enable JavaScript!
Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] There should be some charts here, you may need to enable JavaScript!
BB1 receptor in Human [GtoPdb: 38] [UniProtKB: P28336] There should be some charts here, you may need to enable JavaScript!
BB2 receptor in Human [GtoPdb: 39] [UniProtKB: P30550] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
BB3 receptor/Bombesin receptor subtype-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4080] [GtoPdb: 40] [UniProtKB: P32247]
GtoPdb	-	-	8.43	pKi	-	-	-	Pharmacol Exp Therap (2013) 347: 100-116 [PMID:23892571]; ACS Med Chem Lett (2011) 2: 43-7 [PMID:24900253]
ChEMBL	Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3	B	8.43	pKi	3.7	nM	Ki	ACS Med Chem Lett (2011) 2: 43-47 [PMID:24900253]
ChEMBL	Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assay	F	6.97	pIC50	105.93	nM	IC50	J Med Chem (2023) 66: 8011-8029 [PMID:37272653]
ChEMBL	Displacement of [125I]-[D-Tyr6,beta-Ala11,Phe13,Nle14]-Bombesin (6-14) from human BRS-3	B	7.57	pIC50	27	nM	IC50	ACS Med Chem Lett (2011) 2: 43-47 [PMID:24900253]
GtoPdb	-	-	7.57	pIC50	27	nM	IC50	Pharmacol Exp Therap (2013) 347: 100-116 [PMID:23892571]; ACS Med Chem Lett (2011) 2: 43-7 [PMID:24900253]
ChEMBL	Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assay	F	7.63	pIC50	23.6	nM	IC50	J Med Chem (2023) 66: 8011-8029 [PMID:37272653]
GtoPdb	-	-	7.6	pEC50	25	nM	EC50	ACS Med Chem Lett (2011) 2: 43-7 [PMID:24900253]
ChEMBL	Agonist activity at human BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay	F	7.85	pEC50	14	nM	EC50	ACS Med Chem Lett (2011) 2: 43-47 [PMID:24900253]
ChEMBL	Agonist activity at human BRS3 expressed in CHO-K1 cells by IP-One HTRF assay	B	7.85	pEC50	14	nM	EC50	Bioorg Med Chem (2015) 23: 89-104 [PMID:25497965]
ChEMBL	Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assay	F	9.53	pEC50	0.29	nM	EC50	J Med Chem (2023) 66: 8011-8029 [PMID:37272653]
ChEMBL	Agonist activity at human BB3 stably overexpressed in human NCI-H1299 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay	F	9.68	pEC50	0.21	nM	EC50	J Med Chem (2023) 66: 8011-8029 [PMID:37272653]
BB3 receptor/Bombesin receptor subtype-3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075140] [GtoPdb: 40] [UniProtKB: O54798]
ChEMBL	Displacement of [3H]Bag-3 from mouse BRS-3	B	8.8	pKi	1.6	nM	Ki	ACS Med Chem Lett (2011) 2: 43-47 [PMID:24900253]
GtoPdb	-	-	8.8	pKi	1.6	nM	Ki	J Pharmacol Exp Ther (2011) 336: 356-64 [PMID:21036912]
ChEMBL	Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced IP-1 accumulation by measuring Bantag-1 pIC50 in presence of Bantag-1 incubated for 60 mins by HTRF assay	F	7.71	pIC50	19.41	nM	IC50	J Med Chem (2023) 66: 8011-8029 [PMID:37272653]
ChEMBL	Displacement of [3H]Bag-3 from mouse BRS-3	B	8.27	pIC50	5.4	nM	IC50	ACS Med Chem Lett (2011) 2: 43-47 [PMID:24900253]
ChEMBL	Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as blockade of compound induced intracellular calcium response by measuring Bantag-1 pIC50 preincubated for 10 mins with Bantag-1 followed by compound addition and measured for 3 mins by FLIPR calcium 6 assay	F	8.37	pIC50	4.26	nM	IC50	J Med Chem (2023) 66: 8011-8029 [PMID:37272653]
ChEMBL	Agonist activity at mouse BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay	F	7.68	pEC50	21	nM	EC50	ACS Med Chem Lett (2011) 2: 43-47 [PMID:24900253]
ChEMBL	Agonist activity at mouse BRS3 expressed in CHO-K1 cells by IP-One HTRF assay	B	7.68	pEC50	21	nM	EC50	Bioorg Med Chem (2015) 23: 89-104 [PMID:25497965]
ChEMBL	Agonist activity at endogenous mouse BB3 in mouse B16 cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay	F	7.87	pEC50	13.46	nM	EC50	J Med Chem (2023) 66: 8011-8029 [PMID:37272653]
ChEMBL	Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in intracellular calcium response and measured for 3 mins by FLIPR calcium 6 assay	F	8.52	pEC50	2.99	nM	EC50	J Med Chem (2023) 66: 8011-8029 [PMID:37272653]
ChEMBL	Agonist activity at mouse BB3 stably overexpressed in human HEK cells assessed as increase in IP-1 accumulation incubated for 60 mins by HTRF assay	F	9.38	pEC50	0.42	nM	EC50	J Med Chem (2023) 66: 8011-8029 [PMID:37272653]
BB3 receptor/Bombesin receptor subtype-3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075111] [GtoPdb: 40] [UniProtKB: Q8K418]
ChEMBL	Displacement of [3H]Bag-3 from rat BRS-3	B	9.22	pKi	0.6	nM	Ki	ACS Med Chem Lett (2011) 2: 43-47 [PMID:24900253]
ChEMBL	Displacement of [3H]Bag-3 from rat BRS-3	B	8.92	pIC50	1.2	nM	IC50	ACS Med Chem Lett (2011) 2: 43-47 [PMID:24900253]
ChEMBL	Agonist activity at rat BRS-3 expressed in HEK293AEQ cells assessed as induction of intracellular calcium mobilization by aequorin bioluminescence assay	F	8.66	pEC50	2.2	nM	EC50	ACS Med Chem Lett (2011) 2: 43-47 [PMID:24900253]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL	Binding affinity to human ERG	B	5.1	pKi	>8000	nM	Ki	ACS Med Chem Lett (2011) 2: 43-47 [PMID:24900253]
BB1 receptor in Human [GtoPdb: 38] [UniProtKB: P28336]
GtoPdb	-	-	5	pIC50	>10000	nM	IC50	Pharmacol Exp Therap (2013) 347: 100-116 [PMID:23892571]; J Pharmacol Exp Ther (2011) 336: 356-64 [PMID:21036912]
BB2 receptor in Human [GtoPdb: 39] [UniProtKB: P30550]
GtoPdb	-	-	5	pIC50	>10000	nM	IC50	Pharmacol Exp Therap (2013) 347: 100-116 [PMID:23892571]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]