(S)-dimetindene [Ligand Id: 10104] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1493369
  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
  • 7.16
1 CHEMBL1493369_lig_chart_1 Histamine H1 receptor Human
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
  • 6.72
2 CHEMBL1493369_lig_chart_2 Muscarinic acetylcholine receptor M1 Human
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
  • 7.52
3 CHEMBL1493369_lig_chart_3 Muscarinic acetylcholine receptor M2 Human
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
  • 6.86
4 CHEMBL1493369_lig_chart_4 Muscarinic acetylcholine receptor M3 Human
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
  • 6.53
5 CHEMBL1493369_lig_chart_5 Muscarinic acetylcholine receptor M4 Human
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
  • 6.12
6 CHEMBL1493369_lig_chart_6 Muscarinic acetylcholine receptor M5 Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
GtoPdb - - 7.16 pKi 69 nM Ki J Med Chem (2003) 46: 856-67 [PMID:12593665]
ChEMBL Compound was evaluated for binding affinity towards cloned human histamine H1 receptors stably expressed in CHO-K1 cells using [3H]mepyramine B 7.16 pKi 69.18 nM Ki J. Med. Chem. (2003) 46: 856-867 [PMID:12593665]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL Binding affinity towards cloned human muscarinic acetylcholine receptor M1 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine B 6.72 pKi 190.55 nM Ki J. Med. Chem. (2003) 46: 856-867 [PMID:12593665]
GtoPdb Binding to hM1 receptors expressed in CHO cells. - 6.72 pKi 190.6 nM Ki J Med Chem (2003) 46: 856-67 [PMID:12593665]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Binding affinity towards cloned human muscarinic acetylcholine receptor M2 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine B 7.52 pKi 30.2 nM Ki J. Med. Chem. (2003) 46: 856-867 [PMID:12593665]
GtoPdb Binding to hM2 receptors expressed in CHO cells. - 7.52 pKi 30.2 nM Ki J Med Chem (2003) 46: 856-67 [PMID:12593665]
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine B 6.86 pKi 138.04 nM Ki J. Med. Chem. (2003) 46: 856-867 [PMID:12593665]
GtoPdb Binding to hM3 receptors expressed in CHO cells. - 6.86 pKi 138 nM Ki J Med Chem (2003) 46: 856-67 [PMID:12593665]
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
GtoPdb Binding to hM4 receptors expressed in CHO cells. - 6.53 pKi 295.1 nM Ki J Med Chem (2003) 46: 856-67 [PMID:12593665]
ChEMBL Binding affinity towards cloned human muscarinic acetylcholine receptor M4 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine B 6.53 pKi 295.12 nM Ki J. Med. Chem. (2003) 46: 856-867 [PMID:12593665]
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL Binding affinity towards cloned human muscarinic acetylcholine receptor M5 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine B 6.12 pKi 758.58 nM Ki J. Med. Chem. (2003) 46: 856-867 [PMID:12593665]
GtoPdb Binding to hM5 receptors expressed in CHO cells. - 6.12 pKi 758.6 nM Ki J Med Chem (2003) 46: 856-67 [PMID:12593665]

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]