compound 38 [PMID: 24915291] [Ligand Id: 8145] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3290148
  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
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  • erb-b2 receptor tyrosine kinase 4/Receptor protein-tyrosine kinase erbB-4 in Human [ChEMBL: CHEMBL3009] [GtoPdb: 1799] [UniProtKB: Q15303]
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  • BLK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase BLK in Human [ChEMBL: CHEMBL2250] [GtoPdb: 1940] [UniProtKB: P51451]
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  • BMX non-receptor tyrosine kinase/Tyrosine-protein kinase BMX in Human [ChEMBL: CHEMBL3834] [GtoPdb: 1942] [UniProtKB: P51813]
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  • Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
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  • IL2 inducible T cell kinase/Tyrosine-protein kinase ITK/TSK in Human [ChEMBL: CHEMBL2959] [GtoPdb: 2046] [UniProtKB: Q08881]
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  • Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
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  • tec protein tyrosine kinase/Tyrosine-protein kinase TEC in Human [ChEMBL: CHEMBL4246] [GtoPdb: 2238] [UniProtKB: P42680]
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  • TXK tyrosine kinase/Tyrosine-protein kinase TXK in Human [ChEMBL: CHEMBL4367] [GtoPdb: 2268] [UniProtKB: P42681]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
GtoPdb - - 8.15 pIC50 7 nM IC50 J Med Chem (2014) 57: 5112-28 [PMID:24915291]
ChEMBL Inhibition of EGFR (unknown origin) after 1 hr by HTRF assay B 8.15 pIC50 7 nM IC50 J Med Chem (2014) 57: 5112-5128 [PMID:24915291]
erb-b2 receptor tyrosine kinase 2/Receptor protein-tyrosine kinase erbB-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1824] [GtoPdb: 2019] [UniProtKB: P04626]
GtoPdb - - 8.15 pIC50 7 nM IC50 J Med Chem (2014) 57: 5112-28 [PMID:24915291]
ChEMBL Inhibition of HER2 (unknown origin) after 1 hr by HTRF assay B 8.15 pIC50 7 nM IC50 J Med Chem (2014) 57: 5112-5128 [PMID:24915291]
erb-b2 receptor tyrosine kinase 4/Receptor protein-tyrosine kinase erbB-4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3009] [GtoPdb: 1799] [UniProtKB: Q15303]
GtoPdb - - 8.48 pIC50 3.3 nM IC50 J Med Chem (2014) 57: 5112-28 [PMID:24915291]
ChEMBL Inhibition of HER4 (unknown origin) after 1 hr by HTRF assay B 8.48 pIC50 3.3 nM IC50 J Med Chem (2014) 57: 5112-5128 [PMID:24915291]
BLK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase BLK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2250] [GtoPdb: 1940] [UniProtKB: P51451]
ChEMBL Inhibition of Blk (unknown origin) after 1 hr by HTRF assay B 8.38 pIC50 4.2 nM IC50 J Med Chem (2014) 57: 5112-5128 [PMID:24915291]
GtoPdb - - 8.38 pIC50 4.2 nM IC50 J Med Chem (2014) 57: 5112-28 [PMID:24915291]
BMX non-receptor tyrosine kinase/Tyrosine-protein kinase BMX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3834] [GtoPdb: 1942] [UniProtKB: P51813]
ChEMBL Inhibition of Bmx (unknown origin) after 1 hr by HTRF assay B 9.15 pIC50 0.71 nM IC50 J Med Chem (2014) 57: 5112-5128 [PMID:24915291]
GtoPdb - - 9.15 pIC50 0.71 nM IC50 J Med Chem (2014) 57: 5112-28 [PMID:24915291]
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
ChEMBL Inhibition of Btk phosphorylation at Tyr551 in human Ramos cells after 1 hr by Western blot analysis B 7.89 pIC50 13 nM IC50 J Med Chem (2014) 57: 5112-5128 [PMID:24915291]
ChEMBL Inhibition of Btk in human Ramos cells assessed as inhibition of PLC-gamma2 phosphorylation at Tyr1217 after 1 hr by Western blot analysis B 7.89 pIC50 13 nM IC50 J Med Chem (2014) 57: 5112-5128 [PMID:24915291]
ChEMBL Inhibition of Btk (unknown origin) after 1 hr by HTRF assay B 8.36 pIC50 <4.4 nM IC50 J Med Chem (2014) 57: 5112-5128 [PMID:24915291]
GtoPdb - - 8.36 pIC50 <4.4 nM IC50 J Med Chem (2014) 57: 5112-28 [PMID:24915291]
IL2 inducible T cell kinase/Tyrosine-protein kinase ITK/TSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2959] [GtoPdb: 2046] [UniProtKB: Q08881]
ChEMBL Inhibition of Itk (unknown origin) after 1 hr by HTRF assay B 4.52 pIC50 >30000 nM IC50 J Med Chem (2014) 57: 5112-5128 [PMID:24915291]
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
ChEMBL Inhibition of Jak3 (unknown origin) after 1 hr by HTRF assay B 5.2 pIC50 6370 nM IC50 J Med Chem (2014) 57: 5112-5128 [PMID:24915291]
tec protein tyrosine kinase/Tyrosine-protein kinase TEC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4246] [GtoPdb: 2238] [UniProtKB: P42680]
GtoPdb - - 8.2 pIC50 6.3 nM IC50 J Med Chem (2014) 57: 5112-28 [PMID:24915291]
ChEMBL Inhibition of Tec (unknown origin) after 1 hr by HTRF assay B 8.2 pIC50 6.3 nM IC50 J Med Chem (2014) 57: 5112-5128 [PMID:24915291]
TXK tyrosine kinase/Tyrosine-protein kinase TXK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4367] [GtoPdb: 2268] [UniProtKB: P42681]
GtoPdb - - 8.85 pIC50 1.4 nM IC50 J Med Chem (2014) 57: 5112-28 [PMID:24915291]
ChEMBL Inhibition of Rlk (unknown origin) after 1 hr by HTRF assay B 8.85 pIC50 1.4 nM IC50 J Med Chem (2014) 57: 5112-5128 [PMID:24915291]

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]