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 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]
