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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL3301625 (AVL-292, Btk inhibitor cc-292, CC-292, Spebrutinib)
There should be some charts here, you may need to enable JavaScript!
  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
There should be some charts here, you may need to enable JavaScript!
  • BMX non-receptor tyrosine kinase/Tyrosine-protein kinase BMX in Human [ChEMBL: CHEMBL3834] [GtoPdb: 1942] [UniProtKB: P51813]
There should be some charts here, you may need to enable JavaScript!
  • Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187]
There should be some charts here, you may need to enable JavaScript!
  • Janus kinase 1/Tyrosine-protein kinase JAK1 in Human [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
There should be some charts here, you may need to enable JavaScript!
  • Janus kinase 2/Tyrosine-protein kinase JAK2 in Human [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
There should be some charts here, you may need to enable JavaScript!
  • Janus kinase 3/Tyrosine-protein kinase JAK3 in Human [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333]
There should be some charts here, you may need to enable JavaScript!
  • LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948]
There should be some charts here, you may need to enable JavaScript!
  • tec protein tyrosine kinase/Tyrosine-protein kinase TEC in Human [ChEMBL: CHEMBL4246] [GtoPdb: 2238] [UniProtKB: P42680]
There should be some charts here, you may need to enable JavaScript!
  • YES proto-oncogene 1, Src family tyrosine kinase in Human [GtoPdb: 2284] [UniProtKB: P07947]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Early activation antigen CD69 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3308911] [UniProtKB: Q07108]
ChEMBL Inhibition of CD69 in human whole blood preincubated for 30 mins followed by anti-human IgD stimulation and measured after 18 to 22 hrs by flow cytometry B 5.51 pIC50 3100 nM IC50 J Med Chem (2022) 65: 1206-1224 [PMID:34734694]
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 BTK phosphorylation in human whole blood assessed as reduction in BTK phosphorylation incubated for 30 mins B 7.4 pIC50 40 nM IC50 J Med Chem (2022) 65: 1206-1224 [PMID:34734694]
ChEMBL Inhibition of recombinant human His-tagged full length BTK expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay B 8.01 pIC50 9.8 nM IC50 Bioorg Med Chem (2020) 28: 115236-115236 [PMID:31843459]
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 BTK expressed in baculovirus in Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate incubated for 1 hr by ADP-Glo assay B 8.67 pIC50 2.12 nM IC50 Bioorg Med Chem (2019) 27: 4124-4142 [PMID:31395509]
ChEMBL Inhibition of human BTK using fluorescein-labeled polyGAT peptide as substrate incubated for 30 mins by FRET assay B 9 pIC50 1 nM IC50 J Med Chem (2022) 65: 1206-1224 [PMID:34734694]
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 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 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 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged JAK1 (850 to 1154 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay B 6 pIC50 >1000 nM IC50 Bioorg Med Chem (2020) 28: 115236-115236 [PMID:31843459]
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674]
ChEMBL Inhibition of recombinant human N-terminal His-tagged JAK2 (826 to 1132 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay B 6.27 pIC50 533.7 nM IC50 Bioorg Med Chem (2020) 28: 115236-115236 [PMID:31843459]
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 human N-terminal GST-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins in presence of ATP by ADP-Glo kinase assay B 7.18 pIC50 66.5 nM IC50 Bioorg Med Chem (2020) 28: 115254-115254 [PMID:31866272]
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]
ChEMBL Inhibition of recombinant human N-terminal His-tagged JAK3 (795 to 1124 residues) expressed in baculovirus expression system using Ulight-Poly GT as substrate incubated for 2 hrs by Lanthascreen TR-FRET assay B 8.07 pIC50 8.5 nM IC50 Bioorg Med Chem (2020) 28: 115236-115236 [PMID:31843459]
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 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]