GW803430 [Ligand Id: 4033] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL214957 (GW803430, GW3430)
  • Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
  • This target only has 0 pki data point
  • 0
1 CHEMBL214957_lig_chart_1 HERG Human
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  • H3 receptor/Histamine H3 receptor in Human [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
  • This target only has 1 pki data point
  • 6.68
2 CHEMBL214957_lig_chart_2 Histamine H3 receptor Human
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  • MCH1 receptor/Melanin-concentrating hormone receptor 1 in Human [ChEMBL: CHEMBL344] [GtoPdb: 280] [UniProtKB: Q99705]
  • MCH1 receptor/Melanin-concentrating hormone receptor 1 in Rat [ChEMBL: CHEMBL1075228] [GtoPdb: 280] [UniProtKB: P97639]
  • 9.47
3 CHEMBL214957_lig_chart_3 Melanin-concentrating hormone receptor 1 HumanRat
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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]astemizole from human ERG expressed in HEK293 cells B 5.93 pIC50 1170 nM IC50 J. Med. Chem. (2009) 52: 2076-2089 [PMID:19290642]
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1]
ChEMBL Displacement of [3H]-N-alpha-methylhistamine from human H3R expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting analysis B 6.68 pKi 208 nM Ki ACS Med Chem Lett (2017) 8: 648-653 [PMID:28626527]
MCH1 receptor/Melanin-concentrating hormone receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL344] [GtoPdb: 280] [UniProtKB: Q99705]
ChEMBL Displacement of [3H]GW803430 from MCH-1 receptor expressed in CHO-K1 cells B 8.55 pKi 2.8 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 7020-7023 [PMID:20951036]
ChEMBL Antagonist activity at MCH1R expressed in CHO cells assessed as intracellular Ca2+ mobilization after 20 mins by FLIPR assay F 7.05 pIC50 89.13 nM IC50 J. Med. Chem. (2009) 52: 2076-2089 [PMID:19290642]
ChEMBL Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay B 7.8 pIC50 16 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 2793-2799 [PMID:26022839]
ChEMBL Antagonist activity against human MCHR1 expressed in CHO cells by luciferase reporter gene assay F 9.3 pIC50 0.5 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 4723-4727 [PMID:16870432]
ChEMBL Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay F 9.3 pIC50 0.5 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 6166-6171 [PMID:19773162]
GtoPdb - - 9.3 pIC50 - - - Bioorg Med Chem Lett (2006) 16: 4723-7 [PMID:16870432]
MCH1 receptor/Melanin-concentrating hormone receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075228] [GtoPdb: 280] [UniProtKB: P97639]
ChEMBL Antagonist activity at rat MCHR1 B 9.47 pKi 0.34 nM Ki Bioorg. Med. Chem. Lett. (2015) 25: 2793-2799 [PMID:26022839]

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]