ifidancitinib [Ligand Id: 10638] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4594441 (A-301, Ati-502, ATI-502, Ifidancitinib) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 signaling pathway in human primary T-cells assessed as reduction of IFN-alpha induced STAT1 phosphorylation | B | 8.1 | pIC50 | 8 | nM | IC50 | ACS Med Chem Lett (2022) 13: 1805-1811 [PMID:36385926] |
| Janus kinase 2/Janus kinase 1/JAK2/JAK1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038492] [GtoPdb: 2048, 2047] [UniProtKB: O60674, P23458] | ||||||||
| ChEMBL | Inhibition of JAK1/JAK2 signaling pathway in human U-937 cells assessed as reduction of IFN-gamma induced ICAM1 expression | B | 6.38 | pIC50 | 417 | nM | IC50 | ACS Med Chem Lett (2022) 13: 1805-1811 [PMID:36385926] |
| Janus kinase 2/tyrosine kinase 2/JAK2/TYK2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3301392] [GtoPdb: 2048, 2269] [UniProtKB: O60674, P29597] | ||||||||
| ChEMBL | Inhibition of JAK2/TYK2 signaling pathway in human primary T-cells assessed as reduction of IL-12 induced STAT4 phosphorylation | B | 5.92 | pIC50 | 1189 | nM | IC50 | ACS Med Chem Lett (2022) 13: 1805-1811 [PMID:36385926] |
| 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 signaling pathway in human whole blood assessed as reduction of IL-2 induced STAT5 phosphorylation | B | 6.35 | pIC50 | 451 | nM | IC50 | ACS Med Chem Lett (2022) 13: 1805-1811 [PMID:36385926] |
| ChEMBL | Inhibition of JAK1/JAK3 in human primary T-cells assessed as reduction of IL-2 stimulated STAT5 phosphorylation preincubated for 1 hr followed by IL-2 stimulation for 15 mins by FACS method | B | 7.7 | pIC50 | 20 | nM | IC50 | ACS Med Chem Lett (2022) 13: 1805-1811 [PMID:36385926] |
| ChEMBL | Inhibition of JAK1/JAK3 signaling pathway in human primary T-cells assessed as reduction of IL-2 induced cell proliferation | B | 7.7 | pIC50 | 20 | nM | IC50 | ACS Med Chem Lett (2022) 13: 1805-1811 [PMID:36385926] |
| Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458] | ||||||||
| ChEMBL | Inhibition of human recombinant GST-tagged JAK1 catalytic domain (866 to 1154 residues) expressed in baculovirus expression system by Z'-lyte assay | B | 8.68 | pIC50 | 2.1 | nM | IC50 | ACS Med Chem Lett (2022) 13: 1805-1811 [PMID:36385926] |
| Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] | ||||||||
| ChEMBL | Inhibition of human recombinant GST-tagged JAK3 catalytic domain (781 to 1124 residues) expressed in baculovirus expression system by Z'-lyte assay | B | 6.03 | pIC50 | 923 | nM | IC50 | ACS Med Chem Lett (2022) 13: 1805-1811 [PMID:36385926] |
| tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597] | ||||||||
| ChEMBL | Inhibition of human recombinant N-terminal GST-tagged TYK2 (833 to 1187 residues) expressed in baculovirus expression system by Z'-lyte assay | B | 7.92 | pIC50 | 12 | nM | IC50 | ACS Med Chem Lett (2022) 13: 1805-1811 [PMID:36385926] |
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]
