spebrutinib [Ligand Id: 7837] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3301625 (Spebrutinib, CC-292, AVL-292)
  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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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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  • Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
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  • LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948]
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  • tec protein tyrosine kinase/Tyrosine-protein kinase TEC in Human [ChEMBL: CHEMBL4246] [GtoPdb: 2238] [UniProtKB: P42680]
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  • YES proto-oncogene 1, Src family tyrosine kinase in Human [GtoPdb: 2284] [UniProtKB: P07947]
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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]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged wild-type EGFR (695 to end residues) expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay B 6.35 pIC50 442 nM IC50 Eur J Med Chem (2017) 131: 107-125 [PMID:28315597]
BMX non-receptor tyrosine kinase/Tyrosine-protein kinase BMX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3834] [GtoPdb: 1942] [UniProtKB: P51813]
ChEMBL Inhibition of full length recombinant human N-terminal GST-tagged BMX expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay B 5.57 pIC50 2665 nM IC50 Eur J Med Chem (2017) 131: 107-125 [PMID:28315597]
Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
ChEMBL Reversible inhibition of full length recombinant human N-terminal His tagged BKT expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 2 to 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay B 7.68 pKi 20.7 nM Ki Eur J Med Chem (2017) 131: 107-125 [PMID:28315597]
ChEMBL Inhibition of full length recombinant human N-terminal His tagged BKT expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay B 8.05 pIC50 9 nM IC50 Eur J Med Chem (2017) 131: 107-125 [PMID:28315597]
ChEMBL Inhibition of BTK (unknown origin) B 8.34 pIC50 4.61 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 1954-1957 [PMID:26976214]
ChEMBL Inhibition of human recombinant full-length N-terminal His-tagged BTK expressed in baculovirus infected Sf9 insect cells measured after 60 mins by ADP-Glo kinase assay B 9.14 pIC50 0.72 nM IC50 Bioorg Med Chem (2017) 25: 765-772 [PMID:27956037]
ChEMBL Inhibition of N-terminal His-tagged full length human recombinant BTK expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) peptide substrate incubated for 60 mins by ADP-Glo luminescence assay B 9.14 pIC50 0.72 nM IC50 Eur J Med Chem (2017) 126: 444-455 [PMID:27912175]
ChEMBL Inhibition of human recombinant full-length N-terminal His-tagged BTK expressed in baculovirus infected Sf9 insect cells after 60 mins by ADP-Glo kinase assay B 9.14 pIC50 0.72 nM IC50 Eur J Med Chem (2017) 135: 60-69 [PMID:28432946]
ChEMBL Inhibition of BTK (unknown origin) B 9.15 pIC50 0.7 nM IC50 Eur J Med Chem (2018) 151: 315-326 [PMID:29631132]
ChEMBL Inhibition of recombinant human N-terminal His-tagged BTK expressed in baculovirus infected sf9 cells using poly(4:1 Glu,Tyr) as substrate by ADP-Glo kinase assay B 9.22 pIC50 0.6 nM IC50 ACS Med Chem Lett (2016) 7: 1050-1055 [PMID:27994736]
ChEMBL Inhibition of recombinant full-length N-terminal His-tagged human BTK expressed in baculovirus infected Sf9 insect cells using Poly(4:1 Glu,Tyr) peptide substrate incubated for 60 mins by ADP-Glo luminescence assay B 9.22 pIC50 0.6 nM IC50 Eur J Med Chem (2018) 143: 1847-1857 [PMID:29146136]
GtoPdb - - 9.3 pIC50 <0.5 nM IC50 Clinical Development of AVL - 292: A Potent, Selective Covalent Btk Inhibitor for the Treatment of B Cell Malignancies.. http://www.celgene.com
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay B 5.76 pIC50 1753 nM IC50 Eur J Med Chem (2017) 131: 107-125 [PMID:28315597]
ChEMBL Inhibition of recombinant N-terminal GST-tagged human JAK3 (781 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly(4:1 Glu,Tyr) peptide substrate incubated for 60 mins by ADP-Glo luminescence assay B 7.65 pIC50 22.5 nM IC50 Eur J Med Chem (2018) 143: 1847-1857 [PMID:29146136]
LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948]
ChEMBL Inhibition of LYN (unknown origin) B 5.36 pIC50 4400 nM IC50 Eur J Med Chem (2018) 151: 315-326 [PMID:29631132]
tec protein tyrosine kinase/Tyrosine-protein kinase TEC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4246] [GtoPdb: 2238] [UniProtKB: P42680]
ChEMBL Inhibition of TEC (unknown origin) B 8.21 pIC50 6.2 nM IC50 Eur J Med Chem (2018) 151: 315-326 [PMID:29631132]
YES proto-oncogene 1, Src family tyrosine kinase in Human [GtoPdb: 2284] [UniProtKB: P07947]
GtoPdb - - 6.14 pIC50 723 nM IC50 Clinical Development of AVL - 292: A Potent, Selective Covalent Btk Inhibitor for the Treatment of B Cell Malignancies.. http://www.celgene.com

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]