Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL4213248 |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
---|---|---|---|---|---|---|---|---|
coagulation factor X/Coagulation factor X in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL244] [GtoPdb: 2359] [UniProtKB: P00742] | ||||||||
ChEMBL | Inhibition of factor 10a (unknown origin) using chromogenic H-D-Ile-L-Pro-L-Arg-p-nitoraniline as substrate by fluorescence assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2018) 61: 8299-8320 [PMID:30130401] |
coagulation factor XI/Coagulation factor XI in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2820] [GtoPdb: 2360] [UniProtKB: P03951] | ||||||||
ChEMBL | Inhibition of factor 11a (unknown origin) using chromogenic L-pyroGlu-L-Pro-L-Arg-p-nitroaniline as substrate by fluorescence assay | B | 4.51 | pIC50 | 31000 | nM | IC50 | J Med Chem (2018) 61: 8299-8320 [PMID:30130401] |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Inhibition of recombinant human ERG expressed in CHO cells incubated for 12 mins by whole cell voltage clamp method | B | 5.52 | pIC50 | <3000 | nM | IC50 | Bioorg Med Chem (2021) 37: 116116-116116 [PMID:33799173] |
kallikrein B1/Plasma kallikrein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2000] [GtoPdb: 2379] [UniProtKB: P03952] | ||||||||
ChEMBL | Inhibition of human plasma kallikrein using chromogenic L-pyroGlu-L-Pro-L-Arg-p-nitroaniline as substrate by fluorescence assay | B | 4.95 | pIC50 | 11300 | nM | IC50 | J Med Chem (2018) 61: 8299-8320 [PMID:30130401] |
plasminogen/Plasminogen in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1801] [GtoPdb: 2394] [UniProtKB: P00747] | ||||||||
ChEMBL | Inhibition of plasmin (unknown origin) using chromogenic H-D-Ile-L-Pro-L-Arg-p-nitoraniline as substrate by fluorescence assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2018) 61: 8299-8320 [PMID:30130401] |
Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524] | ||||||||
ChEMBL | Inhibition of recombinant human Nav1.5alpha expressed in HEK293 cells incubated for 10 mins by voltage clamp method | B | 5.52 | pIC50 | <3000 | nM | IC50 | Bioorg Med Chem (2021) 37: 116116-116116 [PMID:33799173] |
coagulation factor II, thrombin/Thrombin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734] | ||||||||
ChEMBL | Inhibition of thrombin (unknown origin) using chromogenic H-D-Ile-L-Pro-L-Arg-p-nitoraniline as substrate by fluorescence assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2018) 61: 8299-8320 [PMID:30130401] |
plasminogen activator, tissue type/Tissue-type plasminogen activator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1873] [GtoPdb: 2392] [UniProtKB: P00750] | ||||||||
ChEMBL | Inhibition of tPA (unknown origin) using chromogenic H-D-Ile-L-Pro-L-Arg-p-nitoraniline as substrate by fluorescence assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2018) 61: 8299-8320 [PMID:30130401] |
plasminogen activator, urokinase/Urokinase-type plasminogen activator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3286] [GtoPdb: 2393] [UniProtKB: P00749] | ||||||||
ChEMBL | Inhibition of human kidney uPA using Z-Gly-Gly-Arg-AMC as substrate measured over 15 mins by fluorescence assay | B | 6.74 | pKi | 183 | nM | Ki | J Med Chem (2018) 61: 8299-8320 [PMID:30130401] |
GtoPdb | - | - | 6.74 | pKi | 183 | nM | Ki | J Med Chem (2018) 61: 8299-8320 [PMID:30130401] |
ChEMBL | Inhibition of human kidney uPA using chromogenic H-D-Ile-L-Pro-L-Arg-p-nitoraniline as substrate by fluorescence assay | B | 6.28 | pIC50 | 530 | nM | IC50 | J Med Chem (2018) 61: 8299-8320 [PMID:30130401] |
plasminogen activator, urokinase/Urokinase-type plasminogen activator in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075311] [GtoPdb: 2393] [UniProtKB: P06869] | ||||||||
ChEMBL | Inhibition of mouse uPA using Z-Gly-Gly-Arg-AMC as substrate after 15 mins by fluorescence assay | B | 5.74 | pKi | 1802 | nM | Ki | J Med Chem (2018) 61: 8299-8320 [PMID:30130401] |
protein C, inactivator of coagulation factors Va and VIIIa/Vitamin K-dependent protein C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4444] [GtoPdb: 2396] [UniProtKB: P04070] | ||||||||
ChEMBL | Inhibition of activated protein C (unknown origin) using chromogenic L-pyroGlu-L-Pro-L-Arg-p-nitroaniline as substrate by fluorescence assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2018) 61: 8299-8320 [PMID:30130401] |
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]