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ChEMBL ligand: CHEMBL4447181 (Londamocitinib) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | WO2018134213A1. Jak1 selective inhibitors (2018) |
ChEMBL | Inhibition of N-terminal GST-tagged human recombinant JAK1 (866 to 1154 residues) expressed in insect cells using FITC-C6-KKHTDDGYMPMSPGVA-NH peptide as substrate incubated for 10 mins measured after 90 mins in presence of ATP by caliper mobility shift assay | B | 8.52 | pIC50 | <3 | nM | IC50 | J Med Chem (2023) 66: 13400-13415 [PMID:37738648] |
ChEMBL | Inhibition of GST-tagged human recombinant JAK1 (866 to 1154 residues) expressed in insect cells | B | 9.27 | pIC50 | 0.54 | nM | IC50 | J Med Chem (2023) 66: 13400-13415 [PMID:37738648] |
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
GtoPdb | - | - | 5.91 | pIC50 | 1220 | nM | IC50 | WO2018134213A1. Jak1 selective inhibitors (2018) |
ChEMBL | Inhibition of N-terminal GST-tagged human recombinant JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 peptide as substrate incubated for 10 mins measured after 90 mins in presence of ATP by caliper mobility shift assay | B | 5.91 | pIC50 | 1221 | nM | IC50 | J Med Chem (2023) 66: 13400-13415 [PMID:37738648] |
ChEMBL | Inhibition of GST-tagged human recombinant JAK2 (809 to 1153 residues) expressed in insect cells | B | 6.16 | pIC50 | 686 | nM | IC50 | J Med Chem (2023) 66: 13400-13415 [PMID:37738648] |
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] | ||||||||
ChEMBL | Inhibition of N-terminal GST-tagged human recombinant JAK3 (781 to 1124 residues) expressed in insect cells using 5FAM-GEEPLYWSFPAKKK-NH2 peptide as substrate incubated for 10 mins measured after 90 mins in presence of ATP by caliper mobility shift assay | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2023) 66: 13400-13415 [PMID:37738648] |
ChEMBL | Inhibition of GST-tagged human recombinant JAK3 (781 to 1124 residues) expressed in insect cells | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2023) 66: 13400-13415 [PMID:37738648] |
tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597] | ||||||||
ChEMBL | Inhibition of GST-tagged human recombinant TYK2 (833 to 1187 residues) expressed in insect cells | B | 6.18 | pIC50 | 657 | nM | IC50 | J Med Chem (2023) 66: 13400-13415 [PMID:37738648] |
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]