NF449 [Ligand Id: 4267] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1253351 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Meprin A subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105879] [UniProtKB: Q16820] | ||||||||
| ChEMBL | Inhibition of recombinant human meprin beta expressed in baculovirus infected Sf9 insect cells using (MCA)-EDEDED-(K-epsilon-dnp) as substrate by fluorescence assay | B | 7.66 | pKi | 22 | nM | Ki | Bioorg Med Chem Lett (2017) 27: 2428-2431 [PMID:28408220] |
| P2X1/P2X purinoceptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2094] [GtoPdb: 478] [UniProtKB: P51575] | ||||||||
| GtoPdb | - | - | 6.3 | pIC50 | ~500 | nM | IC50 | Eur J Med Chem (2004) 39: 345-57 [PMID:15072843] |
| ChEMBL | Antagonist activity at non-desensitizing human P2X1 receptor ( P2X2/P2X1 chimera) expressed in human 1321N1 cells assessed as inhibition of ATP-induced calcium influx pre-incubated for 30 mins before ATP stimulation by FLIPR assay relative to control | B | 6.63 | pIC50 | 236 | nM | IC50 | J Med Chem (2020) 63: 6164-6178 [PMID:32345019] |
| P2X1/P2X purinoceptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2530] [GtoPdb: 478] [UniProtKB: P47824] | ||||||||
| ChEMBL | Antagonist activity at rat P2X1 receptor | B | 9.55 | pIC50 | 0.28 | nM | IC50 | J Med Chem (2020) 63: 6164-6178 [PMID:32345019] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| Signal transducer and activator of transcription 1-alpha/beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6101] [UniProtKB: P42224] | ||||||||
| ChEMBL | Inhibition of 5-carboxyfluorescein-GpYDKPHVL-OH binding to STAT1 (unknown origin) pre-incubated for 1 hr before fluorescent-labelled peptide addition by fluorescence polarization assay | B | 5.1 | pIC50 | 7900 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3349-3352 [PMID:28624143] |
| signal transducer and activator of transcription 3/Signal transducer and activator of transcription 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5402] [GtoPdb: 2994] [UniProtKB: P42227] | ||||||||
| ChEMBL | Inhibition of 5-carboxyfluorescein-GpYLPQTV-NH2 binding to mouse STAT3 (127 to 722 residues) expressed in Escherichia coli Rosetta BL21 DE3 pre-incubated for 1 hr before fluorescent-labelled peptide addition by fluorescence polarization assay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3349-3352 [PMID:28624143] |
| signal transducer and activator of transcription 5A/Signal transducer and activator of transcription 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5403] [GtoPdb: 3221] [UniProtKB: P42229] | ||||||||
| ChEMBL | Inhibition of 5-carboxyfluorescein-GpYLVLDKW-OH binding to C-terminal 6x-His-tagged and an N-terminal maltose-binding protein-tagged STAT5A SH2 domain (137 to 507 residues) (unknown origin) expressed in Escherichia coli Rosetta BL21 DE3 pre-incubated for 1 hr before fluorescent-labelled peptide addition by fluorescence polarization assay | B | 5.85 | pIC50 | 1400 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3349-3352 [PMID:28624143] |
| Signal transducer and activator of transcription 5B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5817] [UniProtKB: P51692] | ||||||||
| ChEMBL | Inhibition of 5-carboxyfluorescein-GpYLVLDKW-OH binding to STAT5B SH2 domain (unknown origin) pre-incubated for 1 hr before fluorescent-labelled peptide addition by fluorescence polarization assay | B | 5.6 | pIC50 | 2500 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3349-3352 [PMID:28624143] |
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]
