MK-5046 [Ligand Id: 6170] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1672354 (MK-5046) |
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| 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 | 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] |
| 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] |
| 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 | 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 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] |
| 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]
