A-317567 [Ligand Id: 4116] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL185515 (A-317567)
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  • ASIC3 in Human [GtoPdb: 686] [UniProtKB: Q9UHC3]
  • ASIC3/Amiloride-sensitive cation channel 3 in Rat [ChEMBL: CHEMBL5757] [GtoPdb: 686] [UniProtKB: O35240]
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  • plasminogen activator, tissue type/Tissue-type plasminogen activator in Human [ChEMBL: CHEMBL1873] [GtoPdb: 2392] [UniProtKB: P00750]
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  • plasminogen activator, urokinase/Urokinase-type plasminogen activator in Human [ChEMBL: CHEMBL3286] [GtoPdb: 2393] [UniProtKB: P00749]
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  • ASIC2 in Human [GtoPdb: 685] [UniProtKB: Q16515]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ASIC1/Acid-sensing ion channel 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3562170] [GtoPdb: 684] [UniProtKB: P55926]
ChEMBL Inhibition of ASIC1a in rat dorsal root ganglion neurons assessed as reduction in peak current preincubated for 120 secs followed by acid medium stimulation at pH 5.5 for 3 secs by automated patch clamp electrophysiology assay B 5.7 pIC50 2000 nM IC50 Bioorg Med Chem (2018) 26: 3158-3165 [PMID:29699911]
GtoPdb - - 5.7 pIC50 ~2000 nM IC50 Pain (2005) 117: 88-96 [PMID:16061325]
ASIC3 in Human [GtoPdb: 686] [UniProtKB: Q9UHC3]
GtoPdb Human ASIC3 expressed in HEK293 cells - 5.99 pIC50 1025 nM IC50 ACS Chem Neurosci (2010) 1: 19-24 [PMID:22778804]
ASIC3/Amiloride-sensitive cation channel 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5757] [GtoPdb: 686] [UniProtKB: O35240]
ChEMBL Inhibition of ASIC3 in rat DRG neurons B 5.02 pIC50 9500 nM IC50 J. Med. Chem. (2013) 56: 593-624 [PMID:23121096]
kallikrein 1/Kallikrein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2319] [GtoPdb: 2865] [UniProtKB: P06870]
ChEMBL Binding affinity value against kallikrein B 6.24 pKi 576 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 93-98 [PMID:15582418]
plasminogen/Plasminogen in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1801] [GtoPdb: 2394] [UniProtKB: P00747]
ChEMBL Binding affinity value against plasmin B 5.89 pKi 1302 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 93-98 [PMID:15582418]
plasminogen activator, tissue type/Tissue-type plasminogen activator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1873] [GtoPdb: 2392] [UniProtKB: P00750]
ChEMBL Binding affinity value against Tissue plasminogen activator B 5.21 pKi 6230 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 93-98 [PMID:15582418]
Trypsin in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366] [UniProtKB: P00761]
ChEMBL Binding affinity value against trypsin B 7.05 pKi 90 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 93-98 [PMID:15582418]
plasminogen activator, urokinase/Urokinase-type plasminogen activator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3286] [GtoPdb: 2393] [UniProtKB: P00749]
ChEMBL Inhibition of urokinase B 7.3 pKi 50.12 nM Ki J. Med. Chem. (2009) 52: 3159-3165 [PMID:19385614]
ChEMBL Binding affinity value against urokinase plasminogen activator B 7.33 pKi 47 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 93-98 [PMID:15582418]
ASIC2 in Human [GtoPdb: 685] [UniProtKB: Q16515]
GtoPdb - - 4.5 pIC50 ~30000 nM IC50

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]