blovacitinib [Ligand Id: 14046] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL5172397 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Janus kinase 2/Janus kinase 1/tyrosine kinase 2/JAK1/JAK2/TYK2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301390] [GtoPdb: 2048, 2047, 2269] [UniProtKB: O60674, P23458, P29597] | ||||||||
| ChEMBL | Inhibition of JAK1/JAK2/TYK2 signalling in human whole blood assessed as inhibition of IL-6 stimulated STAT1 phosphorylation in CD4+ lymphocytes preincubated for 1 hr followed by IL-6 stimulation and incubated for 20 mins by flow cytometry analysis | B | 6.9 | pIC50 | 125.9 | nM | IC50 | J Med Chem (2022) 65: 16716-16740 [PMID:36512734] |
| GtoPdb | - | - | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2022) 65: 16716-16740 [PMID:36512734] |
| Janus kinase 1/tyrosine kinase 2/JAK1/TYK2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301391] [GtoPdb: 2047, 2269] [UniProtKB: P23458, P29597] | ||||||||
| ChEMBL | Inhibition of JAK1/TYK2 signalling in human whole blood assessed as inhibition of IFN-alpha stimulated STAT1 phosphorylation in CD4+ lymphocytes preincubated for 1 hr followed by IFN-alpha stimulation and incubated for 20 mins by flow cytometry analysis | B | 7.22 | pIC50 | 59.6 | nM | IC50 | J Med Chem (2022) 65: 16716-16740 [PMID:36512734] |
| GtoPdb | - | - | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2022) 65: 16716-16740 [PMID:36512734] |
| Janus kinase 1/Janus kinase 3/JAK3/JAK1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038491] [GtoPdb: 2047, 2049] [UniProtKB: P23458, P52333] | ||||||||
| ChEMBL | Inhibition of JAK1/JAK3 signalling in human whole blood assessed as inhibition of IL-2 stimulated STAT5 phosphorylation in CD4+ lymphocytes preincubated for 1 hr followed by IL-2 stimulation and incubated for 20 mins by flow cytometry analysis | B | 6.8 | pIC50 | 157.4 | nM | IC50 | J Med Chem (2022) 65: 16716-16740 [PMID:36512734] |
| GtoPdb | - | - | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2022) 65: 16716-16740 [PMID:36512734] |
| Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458] | ||||||||
| GtoPdb | - | - | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2022) 65: 16716-16740 [PMID:36512734] |
| ChEMBL | Inhibition of recombinant human JAK1 using MGEEPLYWSFPAKKK as substrate incubated for 40 mins in presence of Mg/ATP mixture by [gamma p33]-ATP based scintillation counting method | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2022) 65: 16716-16740 [PMID:36512734] |
| Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
| ChEMBL | Inhibition of JAK2 signalling in human whole blood assessed as inhibition of GM-CSF stimulated STAT5 phosphorylation in CD33+ monocytes preincubated for 1 hr followed by GM-CSF stimulation and incubated for 20 mins by flow cytometry analysis | B | 5.33 | pIC50 | 4645.2 | nM | IC50 | J Med Chem (2022) 65: 16716-16740 [PMID:36512734] |
| ChEMBL | Inhibition of recombinant human JAK2 using KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWC as substrate incubated for 40 mins in presence of Mg/ATP mixture by [gamma p33]-ATP based scintillation counting method | B | 7.43 | pIC50 | 37 | nM | IC50 | J Med Chem (2022) 65: 16716-16740 [PMID:36512734] |
| Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] | ||||||||
| ChEMBL | Inhibition of recombinant human JAK3 using GGEEEEYFELVKKKK as substrate incubated for 40 mins in presence of Mg/ATP mixture by [gamma p33]-ATP based scintillation counting method | B | 5.82 | pIC50 | 1517 | nM | IC50 | J Med Chem (2022) 65: 16716-16740 [PMID:36512734] |
| tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597] | ||||||||
| ChEMBL | Inhibition of recombinant human TYK2 using GGMEDIYFEFMGGKKK as substrate incubated for 40 mins in presence of Mg/ATP mixture by [gamma p33]-ATP based scintillation counting method | B | 7.44 | pIC50 | 36 | nM | IC50 | J Med Chem (2022) 65: 16716-16740 [PMID:36512734] |
ChEMBL data shown on this page come from version 35:
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]
