MEL57A [Ligand Id: 6260] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1253475
  • HCN1/Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 1 in Mouse [ChEMBL: CHEMBL1250401] [GtoPdb: 400] [UniProtKB: O88704]
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  • HCN2/Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 2 in Mouse [ChEMBL: CHEMBL1250408] [GtoPdb: 401] [UniProtKB: O88703]
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  • HCN4 in Human [GtoPdb: 403] [UniProtKB: Q9Y3Q4]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
HCN1/Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1250401] [GtoPdb: 400] [UniProtKB: O88704]
ChEMBL Blockade of mouse HCN1 expressed in HEK293 cells at -120 f-current amplitude by patch-clamp electrophysiological assay B 6.22 pEC50 600 nM EC50 J Med Chem (2010) 53: 6773-6777 [PMID:20795648]
GtoPdb - - 6.49 pEC50 320 nM EC50 Br J Pharmacol (2012) 166: 602-16 [PMID:22091830]
HCN2/Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1250408] [GtoPdb: 401] [UniProtKB: O88703]
ChEMBL Blockade of mouse HCN2 expressed in HEK293 cells at -120 f-current amplitude by patch-clamp electrophysiological assay B 4.74 pEC50 18300 nM EC50 J Med Chem (2010) 53: 6773-6777 [PMID:20795648]
GtoPdb - - 4.9 pEC50 12560 nM EC50 Br J Pharmacol (2012) 166: 602-16 [PMID:22091830]
HCN4 in Human [GtoPdb: 403] [UniProtKB: Q9Y3Q4]
GtoPdb - - 4.12 pEC50 75260 nM EC50 Br J Pharmacol (2012) 166: 602-16 [PMID:22091830]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]