(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]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
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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 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]