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 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]