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 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]
