MK-0249 [Ligand Id: 7346] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL476323 (Mk-0249, MK-0249, MK0249) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Displacement of [35S]N-[(4R)-1'-[(2R)-6-cyano-1,2,3,4-tetrahydro-2-naphthalenyl]-3,4-dihydro-4-hydroxyspiro[2H-1-benzopyran-2,4'-piperidin]-6-yl]methanesulfonamide from human ERG in HEK293 cells | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2008) 51: 4780-4789 [PMID:18598020] |
| ChEMBL | Displacement of [3H]dofetilide from human recombinant ERG by Competitive binding assay | B | 5 | pIC50 | 10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 5378-5383 [PMID:21802950] |
| H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
| GtoPdb | - | - | 5 | pKi | >10000 | nM | Ki | Pharmacol Rev (2015) 67: 601-55 [PMID:26084539] |
| ChEMBL | Inhibition of human histamine H1 receptor | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2008) 51: 4780-4789 [PMID:18598020] |
| H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021] | ||||||||
| GtoPdb | - | - | 5 | pKi | >10000 | nM | Ki | Pharmacol Rev (2015) 67: 601-55 [PMID:26084539] |
| ChEMBL | Inhibition of human histamine H2 receptor | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2008) 51: 4780-4789 [PMID:18598020] |
| H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
| ChEMBL | Antagonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced binding of [35S]GTPgammaS binding | F | 9.2 | pKd | 0.63 | nM | Kd | J Med Chem (2008) 51: 4780-4789 [PMID:18598020] |
| ChEMBL | Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in CHO-K1 cells | B | 8.17 | pKi | 6.8 | nM | Ki | J Med Chem (2008) 51: 4780-4789 [PMID:18598020] |
| ChEMBL | Binding affinity to recombinant human H3 receptor | B | 8.17 | pKi | 6.8 | nM | Ki | Eur J Med Chem (2016) 108: 655-662 [PMID:26731168] |
| GtoPdb | - | - | 8.2 | pKi | - | - | - | Pharmacol Rev (2015) 67: 601-55 [PMID:26084539] |
| ChEMBL | Inhibition of human H3 receptor | B | 8.77 | pKi | 1.7 | nM | Ki | J Med Chem (2011) 54: 4781-4792 [PMID:21634396] |
| GtoPdb | - | - | 8.77 | pKi | 1.7 | nM | Ki | J Med Chem (2008) 51: 4780-9 [PMID:18598020] |
| ChEMBL | Displacement of [3H]N-alpha-Methylhistamine from human recombinant H3 receptor expressed in HEK293 cells by competitive binding assay | B | 9.2 | pKi | 0.63 | nM | Ki | Eur J Med Chem (2014) 86: 578-588 [PMID:25218907] |
| ChEMBL | Displacement of [125I]Iodoproxyfan from human recombinant histamine H3 receptor by Competitive binding assay | B | 9.27 | pKi | 0.53 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 5378-5383 [PMID:21802950] |
| ChEMBL | Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding | F | 8.77 | pIC50 | 1.7 | nM | IC50 | J Med Chem (2008) 51: 4780-4789 [PMID:18598020] |
| H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8] | ||||||||
| ChEMBL | Displacement of [3H]N-alpha-methylhistamine from rat histamine H3 receptor expressed in HEK293 cells coexpressed with CRE-beta-lactamase | B | 7.48 | pKi | 33 | nM | Ki | J Med Chem (2008) 51: 4780-4789 [PMID:18598020] |
| H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8] | ||||||||
| GtoPdb | - | - | 5 | pKi | >10000 | nM | Ki | Pharmacol Rev (2015) 67: 601-55 [PMID:26084539] |
| ChEMBL | Inhibition of human histamine H4 receptor | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2008) 51: 4780-4789 [PMID:18598020] |
| Histamine receptor H3 in Rhesus macaque (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5299] [UniProtKB: Q865E1] | ||||||||
| ChEMBL | Displacement of [3H]N-alpha-methylhistamine from rhesus monkey histamine H3 receptor expressed in HEK293T cells | B | 8.37 | pKi | 4.3 | nM | Ki | J Med Chem (2008) 51: 4780-4789 [PMID:18598020] |
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]
