fampridine [Ligand Id: 2416] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL284348 (Ampyra, Ampyra Extended Release, Dalfampridine, EL-970, Fampridine, Fampridine (4-aminopyridine), Fampyra, Neurelan, NSC-15041)
  • Kv1.1/Voltage-gated potassium channel subunit Kv1.1 in Human [ChEMBL: CHEMBL2309] [GtoPdb: 538] [UniProtKB: Q09470]
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  • Kv1.2 in Rat [GtoPdb: 539] [UniProtKB: P63142]
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  • Kv1.4 in Rat [GtoPdb: 541] [UniProtKB: P15385]
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  • Kv1.5 in Human [GtoPdb: 542] [UniProtKB: P22460]
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  • Kv1.7 in Mouse [GtoPdb: 544] [UniProtKB: Q17ST2]
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  • Kv1.8 in Human [GtoPdb: 545] [UniProtKB: Q16322]
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  • Kv2.1 in Rat [GtoPdb: 546] [UniProtKB: P15387]
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  • Kv2.2 in Human [GtoPdb: 547] [UniProtKB: Q92953]
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  • Kv3.1 in Mouse [GtoPdb: 548] [UniProtKB: P15388]
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  • Kv3.2 in Rat [GtoPdb: 549] [UniProtKB: P22462]
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  • Kv3.3 in Rat [GtoPdb: 550] [UniProtKB: Q01956]
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  • Kv4.1 in Human [GtoPdb: 552] [UniProtKB: Q9NSA2]
  • Kv4.1 in Mouse [GtoPdb: 552] [UniProtKB: Q03719]
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  • Kv4.2 in Mouse [GtoPdb: 553] [UniProtKB: Q9Z0V2]
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  • Kv4.3 in Mouse [GtoPdb: 554] [UniProtKB: Q9Z0V1]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv1.1/Voltage-gated potassium channel subunit Kv1.1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2309] [GtoPdb: 538] [UniProtKB: Q09470]
ChEMBL Inhibition of Kv1.1 (unknown origin) B 4.05 pIC50 89000 nM IC50 J Med Chem (2017) 60: 2245-2256 [PMID:28225274]
Kv1.2 in Rat [GtoPdb: 539] [UniProtKB: P63142]
GtoPdb - - 3.2 pKd 590000 nM Kd Mol Pharmacol (1994) 45: 1227-34 [PMID:7517498]
Kv1.4 in Rat [GtoPdb: 541] [UniProtKB: P15385]
GtoPdb - - 1.9 pIC50 12500000 nM IC50 EMBO J (1989) 8: 3235-44 [PMID:2555158]
Kv1.5 in Human [GtoPdb: 542] [UniProtKB: P22460]
GtoPdb - - 3.6 pKd 270000 nM Kd Mol Pharmacol (1994) 45: 1227-34 [PMID:7517498]
Kv1.7 in Mouse [GtoPdb: 544] [UniProtKB: Q17ST2]
GtoPdb - - 3.8 pKd - - - J Gen Physiol (2006) 128: 133-45 [PMID:16801386]
GtoPdb - - 3.6 pIC50 245000 nM IC50 J Biol Chem (1998) 273: 5851-7 [PMID:9488722]
Kv1.8 in Human [GtoPdb: 545] [UniProtKB: Q16322]
GtoPdb - - 2.8 pIC50 1580000 nM IC50 Am J Physiol Renal Physiol (2000) 278: F1013-21 [PMID:10836990]
Kv2.1 in Rat [GtoPdb: 546] [UniProtKB: P15387]
GtoPdb - - 3.3 pIC50 500000 nM IC50 J Gen Physiol (1993) 102: 797-816 [PMID:8301258]
Kv2.2 in Human [GtoPdb: 547] [UniProtKB: Q92953]
GtoPdb - - 2.8 pIC50 1500000 nM IC50 Am J Physiol (1998) 274: G901-11 [PMID:9612272]
Kv3.1 in Mouse [GtoPdb: 548] [UniProtKB: P15388]
GtoPdb - - 4.5 pIC50 29000 nM IC50 Mol Pharmacol (1994) 45: 1227-34 [PMID:7517498]
Kv3.2 in Rat [GtoPdb: 549] [UniProtKB: P22462]
GtoPdb - - 4.6 pIC50 24000 nM IC50 J Physiol (Lond.) (2002) 538: 405-19 [PMID:11790809]
Kv3.3 in Rat [GtoPdb: 550] [UniProtKB: Q01956]
GtoPdb - - 2.9 pIC50 - - - Proc Biol Sci (1992) 248: 9-18 [PMID:1381835]
Kv4.1 in Human [GtoPdb: 552] [UniProtKB: Q9NSA2]
GtoPdb - - 2 pIC50 - - - Genomics (2000) 64: 144-54 [PMID:10729221]
Kv4.1 in Mouse [GtoPdb: 552] [UniProtKB: Q03719]
GtoPdb - - 2 pIC50 - - - Proc Natl Acad Sci USA (2002) 99: 1035-40 [PMID:11805342]
Kv4.2 in Mouse [GtoPdb: 553] [UniProtKB: Q9Z0V2]
GtoPdb - - 2.3 pIC50 - - - Mol Pharmacol (2006) 69: 718-26 [PMID:16317109]
Kv4.3 in Mouse [GtoPdb: 554] [UniProtKB: Q9Z0V1]
GtoPdb - - 2.4 pIC50 - - - Br J Pharmacol (2006) 149: 676-86 [PMID:17016508]

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]