PRX-2904 [Ligand Id: 14036] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4741793
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  • Large conductance calcium-activated potassium channel subfamily M beta member 1 in Human [ChEMBL: CHEMBL5078] [UniProtKB: Q16558]
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  • KNa1.1/Potassium channel subfamily T member 1 in Human [ChEMBL: CHEMBL4739688] [GtoPdb: 385] [UniProtKB: Q5JUK3]
  • KNa1.1/Potassium channel subfamily T member 1 in Mouse [ChEMBL: CHEMBL4739694] [GtoPdb: 385] [UniProtKB: Q6ZPR4]
  • KNa1.1/Potassium channel subfamily T member 1 in Rat [ChEMBL: CHEMBL4739708] [GtoPdb: 385] [UniProtKB: Q9Z258]
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  • KNa1.2/Potassium channel subfamily T member 2 in Human [ChEMBL: CHEMBL4739693] [GtoPdb: 386] [UniProtKB: Q6UVM3]
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  • Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
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  • Kv7.1/Voltage-gated potassium channel subunit Kv7.1 in Human [ChEMBL: CHEMBL1866] [GtoPdb: 560] [UniProtKB: P51787]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG by patch clamp analysis B 4.92 pIC50 11900 nM IC50 ACS Med Chem Lett (2021) 12: 593-602 [PMID:33859800]
Large conductance calcium-activated potassium channel subfamily M beta member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5078] [UniProtKB: Q16558]
ChEMBL Inhibition of BK (unknown origin) by patch clamp analysis B 4.88 pIC50 13200 nM IC50 ACS Med Chem Lett (2021) 12: 593-602 [PMID:33859800]
KNa1.1/Potassium channel subfamily T member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4739688] [GtoPdb: 385] [UniProtKB: Q5JUK3]
ChEMBL Inhibition of recombinant wild type human KNa1.1 expressed in human HEK-TREX cells at -80 mV holding potential by automated patch clamp assay B 7.4 pIC50 40 nM IC50 ACS Med Chem Lett (2021) 12: 593-602 [PMID:33859800]
ChEMBL Inhibition of wild-type human Slack expressed in HEK293 cells measured by automated patch clamp assay B 7.4 pIC50 40 nM IC50 Bioorg Med Chem Lett (2022) 76: 129013-129013 [PMID:36184030]
GtoPdb - - 7.4 pIC50 40 nM IC50 ACS Med Chem Lett (2021) 12: 593-602 [PMID:33859800]
KNa1.1/Potassium channel subfamily T member 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4739694] [GtoPdb: 385] [UniProtKB: Q6ZPR4]
ChEMBL Inhibition of recombinant wild type mouse KNa1.1 expressed in human HEK-TREX cells at -80 mV holding potential by automated patch clamp assay B 6.21 pIC50 622 nM IC50 ACS Med Chem Lett (2021) 12: 593-602 [PMID:33859800]
GtoPdb - - 6.21 pIC50 622 nM IC50 ACS Med Chem Lett (2021) 12: 593-602 [PMID:33859800]
KNa1.1/Potassium channel subfamily T member 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4739708] [GtoPdb: 385] [UniProtKB: Q9Z258]
ChEMBL Inhibition of recombinant rat KNa1.1 expressed in human HEK-TREX cells at -80 mV holding potential by automated patch clamp assay B 6.26 pIC50 545 nM IC50 ACS Med Chem Lett (2021) 12: 593-602 [PMID:33859800]
KNa1.2/Potassium channel subfamily T member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4739693] [GtoPdb: 386] [UniProtKB: Q6UVM3]
ChEMBL Inhibition of KCNT2 (unknown origin) by patch clamp analysis B 4.79 pIC50 16400 nM IC50 ACS Med Chem Lett (2021) 12: 593-602 [PMID:33859800]
Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
ChEMBL Inhibition of human Nav1.5 by patch clamp analysis B 4.38 pIC50 42000 nM IC50 ACS Med Chem Lett (2021) 12: 593-602 [PMID:33859800]
Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
ChEMBL Inhibition of Cav1.2 (unknown origin) by patch clamp analysis B 4.97 pIC50 10700 nM IC50 ACS Med Chem Lett (2021) 12: 593-602 [PMID:33859800]
Kv7.1/Voltage-gated potassium channel subunit Kv7.1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1866] [GtoPdb: 560] [UniProtKB: P51787]
ChEMBL Inhibition of Iks (unknown origin) by patch clamp analysis B 4.73 pIC50 18500 nM IC50 ACS Med Chem Lett (2021) 12: 593-602 [PMID:33859800]

ChEMBL data shown on this page come from version 35:

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]