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 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]