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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
