A-317567 [Ligand Id: 4116] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL185515 (A-317567) |
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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 | Pain (2005) 117: 88-96 [PMID:16061325] |
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]
