MK-0249 [Ligand Id: 7346] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL476323 (Mk-0249, MK0249, MK-0249)
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
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  • H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
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  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
  • H3 receptor/Histamine H3 receptor in Rat [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8]
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  • H4 receptor/Histamine H4 receptor in Human [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
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  • Histamine receptor H3 in Rhesus macaque [ChEMBL: CHEMBL5299] [UniProtKB: Q865E1]
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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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]