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 34:
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]
