NS1619 [Ligand Id: 4272] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL384903 (NS-1619)
  • KCa1.1/Calcium-activated potassium channel subunit alpha-1 in Human [ChEMBL: CHEMBL4304] [GtoPdb: 380] [UniProtKB: Q12791]
  • KCa1.1/Calcium-activated potassium channel subunit alpha-1 in Rat [ChEMBL: CHEMBL5505] [GtoPdb: 380] [UniProtKB: Q62976]
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  • heat shock protein 90 alpha family class A member 1/Heat shock protein HSP 90-alpha in Human [ChEMBL: CHEMBL3880] [GtoPdb: 2905] [UniProtKB: P07900]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
KCa1.1/Calcium-activated potassium channel subunit alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4304] [GtoPdb: 380] [UniProtKB: Q12791]
ChEMBL Activation of BK channel-mediated vasorelaxation activity assessed as reduction in KCl-induced contractile tone B 5.23 pIC50 5888.44 nM IC50 Bioorg Med Chem (2009) 17: 319-325 [PMID:19026552]
KCa1.1/Calcium-activated potassium channel subunit alpha-1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5505] [GtoPdb: 380] [UniProtKB: Q62976]
ChEMBL Activation of BK channel in Wistar rat thoracic aorta assessed as relaxation of KCl-induced contraction B 5.29 pIC50 5128.61 nM IC50 Eur J Med Chem (2008) 43: 2618-2626 [PMID:18400336]
ChEMBL Activation of large-conductance calcium-activated potassium channel-mediated vasorelaxation in endothelium-denuded normotensive Wistar rat thoracic aorta assessed as potassium chloride-induced contractile tension B 5.3 pIC50 5011.87 nM IC50 J Med Chem (2008) 51: 5085-5092 [PMID:18680269]
ChEMBL Induction of BK channel mediated vasorelaxation activity in Kcl-induced contraction in Wistar rat aorta B 5.36 pIC50 4365.16 nM IC50 Eur J Med Chem (2008) 43: 792-799 [PMID:17692999]
heat shock protein 90 alpha family class A member 1/Heat shock protein HSP 90-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3880] [GtoPdb: 2905] [UniProtKB: P07900]
ChEMBL Inhibition of Hsp90alpha ATPase activity by malachite green ATP-ase assay B 4.09 pIC50 81000 nM IC50 Bioorg Med Chem Lett (2010) 20: 7503-7506 [PMID:21106457]
ChEMBL Binding affinity to Hsp90alpha N-terminal ATPase domain by TR-FRET assay based competitive binding assay B 5.48 pIC50 3320 nM IC50 Bioorg Med Chem Lett (2010) 20: 7503-7506 [PMID:21106457]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 4.8 pIC50 15848.93 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5.4 pIC50 3981.07 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 5.4 pIC50 3981.07 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]

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]