ABT-239 [Ligand Id: 1218] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL351231 (ABT-239)
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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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  • H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
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  • H2 receptor in Human [GtoPdb: 263] [UniProtKB: P25021]
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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 [3H]dofetilide from human ERG expressed in HEK293 cells B 6.4 pKi 400 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 3295-3300 [PMID:20457525]
ChEMBL Displacement of [3H]dofetilide from human recombinant ERG by Competitive binding assay B 5.8 pIC50 1600 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 5378-5383 [PMID:21802950]
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 SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs F 7.89 pKd 12.88 nM Kd Eur. J. Med. Chem. (2009) 44: 4413-4425 [PMID:19577344]
ChEMBL Displacement of [3H]-NAMH from human histamine H3 receptor expressed in CHO cells B 8.04 pKi 9.1 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 6126-6130 [PMID:21906941]
ChEMBL Displacement of [3H]NAMH from human histamine H3 receptor expressed in CHO cells B 8.04 pKi 9.1 nM Ki J. Med. Chem. (2011) 54: 4781-4792 [PMID:21634396]
ChEMBL Displacement of [3H]RAMH from human histamine H3 receptor expressed in CHO cells B 8.4 pKi 4 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 4377-4379 [PMID:18606542]
ChEMBL Binding affinity to human histamine H3 receptor B 8.62 pKi 2.4 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 3670-3675 [PMID:17498953]
ChEMBL Binding affinity to human histamine H3 receptor B 8.87 pKi 1.35 nM Ki J. Med. Chem. (2011) 54: 26-53 [PMID:21062081]
ChEMBL Binding potency was determined by displacement of [3H]N-alpha-methyl histamine from cloned human histamine H3 receptor expressed in C6 cells B 9.35 pKi 0.45 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 689-693 [PMID:14741270]
ChEMBL Displacement of [3H]N-alpha-methylhistamine from human cloned histamine H3 receptor B 9.35 pKi 0.45 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 3295-3300 [PMID:20457525]
ChEMBL Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in SK-N-MC cells B 9.35 pKi 0.45 nM Ki Eur. J. Med. Chem. (2009) 44: 4413-4425 [PMID:19577344]
ChEMBL In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing human histamine H3 receptor B 9.35 pKi 0.45 nM Ki J. Med. Chem. (2005) 48: 38-55 [PMID:15634000]
ChEMBL Displacement of [125I]Iodoproxyfan from human recombinant histamine H3 receptor by Competitive binding assay B 9.35 pKi 0.45 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 5378-5383 [PMID:21802950]
ChEMBL In vitro binding affinity for human histamine H3 receptor using [3H]N-alpha-methylhistamine B 9.35 pKi 0.45 nM Ki J. Med. Chem. (2005) 48: 6482-6490 [PMID:16190774]
ChEMBL Displacement of [3H]-N-alpha methyl histamine from human H3 receptor expressed in C6 cells B 9.35 pKi 0.45 nM Ki J. Med. Chem. (2007) 50: 5439-5448 [PMID:17918921]
ChEMBL Displacement of [3H]N-alpha-methylhistamine from human cloned histamine H3 receptor expressed in C6 cells B 9.35 pKi 0.45 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 1443-1446 [PMID:17169555]
ChEMBL Displacement of [3H]N-alpha methyl histamine from human cloned histamine H3 receptor expressed in C6 cells B 9.35 pKi 0.45 nM Ki J. Med. Chem. (2009) 52: 4640-4649 [PMID:19588934]
ChEMBL Displacement of [3H]-N-alpha methyl histamine from human H3 receptor expressed in C6 cells B 9.35 pKi 0.45 nM Ki J. Med. Chem. (2007) 50: 5439-5448 [PMID:17918921]
ChEMBL Displacement of [3H]N-alpha methyl histamine from human cloned histamine H3 receptor expressed in C6 cells B 9.35 pKi 0.45 nM Ki J. Med. Chem. (2009) 52: 4640-4649 [PMID:19588934]
ChEMBL Binding potency was determined by displacement of [3H]N-alpha-methyl histamine from cloned human histamine H3 receptor expressed in C6 cells B 9.35 pKi 0.45 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 689-693 [PMID:14741270]
ChEMBL In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing human histamine H3 receptor B 9.35 pKi 0.45 nM Ki J. Med. Chem. (2005) 48: 38-55 [PMID:15634000]
ChEMBL Binding affinity to histamine H3 receptor B 9.4 pKi 0.4 nM Ki J. Med. Chem. (2009) 52: 3855-3868 [PMID:19456097]
GtoPdb - - 9.4 pKi - - - J Pharmacol Exp Ther (2005) 313: 165-75 [PMID:15608078]
ChEMBL Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding F 9.2 pIC50 0.63 nM IC50 J. Med. Chem. (2008) 51: 6889-6901 [PMID:18841880]
ChEMBL Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding F 8.89 pEC50 1.29 nM EC50 J. Med. Chem. (2007) 50: 5439-5448 [PMID:17918921]
ChEMBL Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding F 8.89 pEC50 1.29 nM EC50 J. Med. Chem. (2007) 50: 5439-5448 [PMID:17918921]
H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8]
ChEMBL Displacement of [3H]NAMH from rat histamine H3 receptor expressed in CHO cells B 7.51 pKi 31 nM Ki J. Med. Chem. (2011) 54: 4781-4792 [PMID:21634396]
ChEMBL Antagonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as inhibition of RAMH-stimulated [35S]GTP-gamma-S binding F 8.34 pKi 4.57 nM Ki J. Med. Chem. (2007) 50: 5439-5448 [PMID:17918921]
ChEMBL Binding potency was determined by displacement of [3H]N-alpha-methyl histamine from histamine H3 receptor of rat cortical membranes B 8.49 pKi 3.24 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 689-693 [PMID:14741270]
ChEMBL Displacement of [3H]N-alpha methyl histamine from rat cortical membrane histamine H3 receptor B 8.49 pKi 3.24 nM Ki J. Med. Chem. (2009) 52: 4640-4649 [PMID:19588934]
ChEMBL Binding potency was determined by displacement of [3H]N-alpha-methyl histamine from histamine H3 receptor of rat cortical membranes B 8.49 pKi 3.22 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 689-693 [PMID:14741270]
ChEMBL Displacement of [3H]N-alpha-methylhistamine from histamine H3 receptor in rat cortical membranes B 8.49 pKi 3.22 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 1443-1446 [PMID:17169555]
ChEMBL Displacement of [3H]N-alpha methyl histamine from rat cortical membrane histamine H3 receptor B 8.49 pKi 3.22 nM Ki J. Med. Chem. (2009) 52: 4640-4649 [PMID:19588934]
ChEMBL Displacement of [3H]-NAMH from rat histamine H3 receptor expressed in CHO cells B 8.52 pKi 3 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 6126-6130 [PMID:21906941]
ChEMBL Displacement of [3H]N-alpha-methylhistamine from rat cloned histamine H3 receptor B 8.85 pKi 1.4 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 3295-3300 [PMID:20457525]
ChEMBL Displacement of [3H]-N-alpha methyl histamine from rat H3 receptor expressed in C6 cells B 8.87 pKi 1.35 nM Ki J. Med. Chem. (2007) 50: 5439-5448 [PMID:17918921]
ChEMBL In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing rat histamine H3 receptor B 8.87 pKi 1.35 nM Ki J. Med. Chem. (2005) 48: 38-55 [PMID:15634000]
ChEMBL In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing rat histamine H3 receptor B 8.87 pKi 1.35 nM Ki J. Med. Chem. (2005) 48: 38-55 [PMID:15634000]
ChEMBL Displacement of [3H]-N-alpha methyl histamine from rat H3 receptor expressed in C6 cells B 8.87 pKi 1.35 nM Ki J. Med. Chem. (2007) 50: 5439-5448 [PMID:17918921]
GtoPdb - - 8.9 pKi - - - J Pharmacol Exp Ther (2005) 313: 165-75 [PMID:15608078]
ChEMBL In vitro binding affinity for rat histamine H3 receptor using [3H]N-alpha-methylhistamine B 8.91 pKi 1.23 nM Ki J. Med. Chem. (2005) 48: 6482-6490 [PMID:16190774]
ChEMBL Binding affinity to rat cortical histamine H3 receptor B 9.35 pKi 0.45 nM Ki J. Med. Chem. (2011) 54: 26-53 [PMID:21062081]
ChEMBL Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding F 7.76 pEC50 17.4 nM EC50 J. Med. Chem. (2007) 50: 5439-5448 [PMID:17918921]
ChEMBL Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding F 7.76 pEC50 17.38 nM EC50 J. Med. Chem. (2007) 50: 5439-5448 [PMID:17918921]
H1 receptor in Human [GtoPdb: 262] [UniProtKB: P35367]
GtoPdb - - 5.8 pKi - - - J Pharmacol Exp Ther (2005) 313: 165-75 [PMID:15608078]
H2 receptor in Human [GtoPdb: 263] [UniProtKB: P25021]
GtoPdb - - 5.2 pKi - - - J Pharmacol Exp Ther (2005) 313: 165-75 [PMID:15608078]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]