londamocitinib [Ligand Id: 11716] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4447181 (Londamocitinib)
  • Janus kinase 1/Tyrosine-protein kinase JAK1 in Human [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
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  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
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  • Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
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  • tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]