dabrafenib [Ligand Id: 6494] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2028663 (GSK2118436A, Gsk2118436, GSK-2118436A, Dabrafenib, GSK-2118436, Tafinlar)
  • dual serine/threonine and tyrosine protein kinase/Dual serine/threonine and tyrosine protein kinase in Human [ChEMBL: CHEMBL1908386] [GtoPdb: 2008] [UniProtKB: Q6XUX3]
  • This target only has 0 pki data point
  • 0
1 CHEMBL2028663_lig_chart_1 Dual serine/threonine and tyrosine protein kinase Human
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  • KRAS/GTPase KRas in Human [ChEMBL: CHEMBL2189121] [GtoPdb: 2824] [UniProtKB: P01116]
  • This target only has 0 pki data point
  • 0
2 CHEMBL2028663_lig_chart_2 GTPase KRas Human
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  • Heat shock factor protein 1 in Human [ChEMBL: CHEMBL5869] [UniProtKB: Q00613]
  • This target only has 0 pki data point
  • 0
3 CHEMBL2028663_lig_chart_3 Heat shock factor protein 1 Human
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  • Pirin in Human [ChEMBL: CHEMBL2010627] [UniProtKB: O00625]
  • This target only has 0 pki data point
  • 0
4 CHEMBL2028663_lig_chart_4 Pirin Human
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  • receptor interacting serine/threonine kinase 1/Receptor-interacting serine/threonine-protein kinase 1 in Human [ChEMBL: CHEMBL5464] [GtoPdb: 2189] [UniProtKB: Q13546]
  • This target only has 0 pki data point
  • 0
5 CHEMBL2028663_lig_chart_5 Receptor-interacting serine/threonine-protein kinase 1 Human
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  • receptor interacting serine/threonine kinase 3/Receptor-interacting serine/threonine-protein kinase 3 in Human [ChEMBL: CHEMBL1795199] [GtoPdb: 2191] [UniProtKB: Q9Y572]
  • This target only has 0 pki data point
  • 0
6 CHEMBL2028663_lig_chart_6 Receptor-interacting serine/threonine-protein kinase 3 Human
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  • A-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase A-Raf in Human [ChEMBL: CHEMBL1169596] [GtoPdb: 1933] [UniProtKB: P10398]
  • This target only has 0 pki data point
  • 0
7 CHEMBL2028663_lig_chart_7 Serine/threonine-protein kinase A-Raf Human
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  • B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056]
  • This target only has 0 pki data point
  • 0
8 CHEMBL2028663_lig_chart_8 Serine/threonine-protein kinase B-raf Human
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  • Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049]
  • This target only has 0 pki data point
  • 0
9 CHEMBL2028663_lig_chart_9 Serine/threonine-protein kinase RAF Human
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  • receptor interacting serine/threonine kinase 2/Serine/threonine-protein kinase RIPK2 in Human [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353]
  • This target only has 0 pki data point
  • 0
10 CHEMBL2028663_lig_chart_10 Serine/threonine-protein kinase RIPK2 Human
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  • transforming growth factor beta receptor 1/TGF-beta receptor type I in Human [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897]
  • This target only has 0 pki data point
  • 0
11 CHEMBL2028663_lig_chart_11 TGF-beta receptor type I Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
dual serine/threonine and tyrosine protein kinase/Dual serine/threonine and tyrosine protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1908386] [GtoPdb: 2008] [UniProtKB: Q6XUX3]
ChEMBL Inhibition of human RIPK5 using MBP as substrate by [gamma33-ATP] based radiometric assay B 4.53 pIC50 29350 nM IC50 J Med Chem (2020) 63: 1490-1510 [PMID:31622096]
KRAS/GTPase KRas in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189121] [GtoPdb: 2824] [UniProtKB: P01116]
ChEMBL Inhibition of KRAS G13D mutant in human HCT116 cells assessed as inhibition of ERK phosphorylation by ELISA B 5.23 pIC50 5880 nM IC50 J. Med. Chem. (2015) 58: 4165-4179 [PMID:25965804]
Heat shock factor protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5869] [UniProtKB: Q00613]
ChEMBL Inhibition of 17-AAG-induced HSF1 pathway in human SKOV3 cells assessed as reduction in HSP72 induction preincubated for 1 hr followed by 17-AAG addition measured after 18 hrs by ELISA B 5 pIC50 >10000 nM IC50 J Med Chem (2017) 60: 180-201 [PMID:28004573]
ChEMBL Inhibition of 17-AAG-induced HSF1 pathway in human SKOV3 cells assessed as reduction in HSP72 induction preincubated for 1 hr followed by 17-AAG addition measured after 18 hrs by ELISA B 5 pIC50 >10000 nM IC50 J Med Chem (2017) 60: 180-201 [PMID:28004573]
Pirin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2010627] [UniProtKB: O00625]
ChEMBL Displacement of 6-amino-9-(2-((4-((2-((6-((5-(2,3-dihydrobenzo[b][1,4]dioxine-6-carboxamido)-2-methylphenyl)carbamoyl)quinolin-2-yl)oxy)ethyl)amino)-4-oxobutyl)(methyl)carbamoyl)phenyl)-3-imino-3H-xanthene-4,5-disulfonic acid from pirin (unknown origin) by fluorescence polarization assay B 5 pIC50 >10000 nM IC50 ACS Med Chem Lett (2018) 9: 1199-1204 [PMID:30613326]
receptor interacting serine/threonine kinase 1/Receptor-interacting serine/threonine-protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5464] [GtoPdb: 2189] [UniProtKB: Q13546]
ChEMBL Inhibition of human RIPK1 using MBP as substrate by [gamma33-ATP] based radiometric assay B 4.27 pIC50 53200 nM IC50 J Med Chem (2020) 63: 1490-1510 [PMID:31622096]
receptor interacting serine/threonine kinase 3/Receptor-interacting serine/threonine-protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795199] [GtoPdb: 2191] [UniProtKB: Q9Y572]
ChEMBL Inhibition of human full length N-terminal GST-tagged RIPK3 expressed in baculovirus infected sf9 insect cells assessed as reduction in MBP phosphorylation using MBP as substrate by kinase-Glo luminescence assay B 6.6 pIC50 250 nM IC50 J Med Chem (2020) 63: 1490-1510 [PMID:31622096]
ChEMBL Inhibition of human RIPK3 using MBP as substrate by [gamma33-ATP] based radiometric assay B 8.7 pIC50 2 nM IC50 J Med Chem (2020) 63: 1490-1510 [PMID:31622096]
A-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase A-Raf in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1169596] [GtoPdb: 1933] [UniProtKB: P10398]
ChEMBL Competitive binding affinity to ARAF in human A375 cells after 15 mins in presence of ATP analogue B 7.59 pIC50 26 nM IC50 J. Med. Chem. (2015) 58: 4165-4179 [PMID:25965804]
B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056]
ChEMBL Inhibition of BRAF V600E mutant in human A375 cells assessed as inhibition of ERK phosphorylation measured after 72 hrs by ELISA assay B 7.96 pIC50 11 nM IC50 J. Med. Chem. (2015) 58: 4165-4179 [PMID:25965804]
ChEMBL Inhibition of wild type BRAF (unknown origin) assessed as ADP formation measured for 5 hrs by pyruvate kinase/lactate dehydrogenase coupled assay in presence of ATP, MEK1, NADH B 8.01 pIC50 9.7 nM IC50 J. Med. Chem. (2015) 58: 4165-4179 [PMID:25965804]
ChEMBL Inhibition of recombinant human N-terminal GST-6His tagged BRAF V600E mutant (417 to 766 residues) expressed in baculovirus infected Sf9 cells preincubated with substrate followed by protein and ATP addition measured after 60 mins by scintillation counter method B 8.05 pIC50 9 nM IC50 ACS Med Chem Lett (2016) 7: 962-966 [PMID:27774137]
ChEMBL Inhibition of B-Raf V600E mutant-driven A375P-F11 cell proliferation F 8.1 pIC50 8 nM IC50 ACS Med. Chem. Lett. (2013) 4: 358-362 [PMID:24900673]
ChEMBL Competitive binding affinity to BRAF in human A375 cells after 15 mins in presence of ATP analogue B 8.22 pIC50 6 nM IC50 J. Med. Chem. (2015) 58: 4165-4179 [PMID:25965804]
ChEMBL Inhibition of recombinant human full length GST-tagged BRAF expressed in baculovirus expression system B 8.3 pIC50 5 nM IC50 ACS Med Chem Lett (2018) 9: 1199-1204 [PMID:30613326]
ChEMBL Inhibition of B-Raf V600E mutant in human HepG2 cells assessed as decrease in ERK phosphorylation B 8.4 pIC50 4 nM IC50 ACS Med. Chem. Lett. (2013) 4: 358-362 [PMID:24900673]
ChEMBL Inhibition of B-Raf V600E mutant in human SK-MEL-28 cells assessed as decrease in ERK phosphorylation incubated for 1 hr by immunoassay B 8.4 pIC50 4 nM IC50 ACS Med. Chem. Lett. (2013) 4: 358-362 [PMID:24900673]
ChEMBL Inhibition of BRAF V600E mutant in human A375 cells assessed as reduction in ERK phosphorylation by Western blot analysis B 8.4 pIC50 4 nM IC50 J Med Chem (2018) 61: 5775-5793 [PMID:29461827]
GtoPdb - - 8.49 pIC50 3.2 nM IC50 Mol Cancer Ther (2009) 8:
ChEMBL Inhibition of B-Raf V600E mutant in human A375 cells assessed as ERK phosphorylation preincubated for 1 hr by Western blot method B 9 pIC50 1 nM IC50 Bioorg. Med. Chem. (2016) 24: 2215-2234 [PMID:27085672]
ChEMBL Inhibition of recombinant human GST-tagged BRAF V600E mutant expressed in baculovirus expression system B 9 pIC50 <1 nM IC50 ACS Med Chem Lett (2018) 9: 1199-1204 [PMID:30613326]
ChEMBL Inhibition of B-Raf V600E mutant (unknown origin) assessed as MEK1 phosphorylation using MEK1-Avitag as substrate after 1 hr by HTRF assay B 9 pIC50 1 nM IC50 Bioorg. Med. Chem. (2016) 24: 2215-2234 [PMID:27085672]
ChEMBL Inhibition of BRAF V600E mutant (unknown origin) B 9.1 pIC50 0.8 nM IC50 J Med Chem (2018) 61: 5775-5793 [PMID:29461827]
ChEMBL Inhibition of B-Raf V600E mutant (unknown origin) using fluorescein-MAP2K1 as substrate after 1 hr by electrophoretic assay B 9.15 pIC50 0.71 nM IC50 MedChemComm (2017) 8: 1835-1844
ChEMBL Inhibition of B-Raf V600E mutant (unknown origin) using fluorescein-MAP2K1 as substrate after 1 hr by electrophoretic assay B 9.15 pIC50 0.7 nM IC50 MedChemComm (2017) 8: 1835-1844
ChEMBL Inhibition of N-terminal His tagged B-Raf V600E mutant (unknown origin) expressed in baculovirus infected insect cells co-expressing CDC37 assessed as decrease in biotinylated-MEK protein phosphorylation by AlphaScreen assay B 9.15 pIC50 0.7 nM IC50 ACS Med. Chem. Lett. (2013) 4: 358-362 [PMID:24900673]
ChEMBL Inhibition of wild type B-Raf (unknown origin) assessed as MEK1 phosphorylation using MEK1-Avitag as substrate after 1 hr by HTRF assay B 9.4 pIC50 0.4 nM IC50 Bioorg. Med. Chem. (2016) 24: 2215-2234 [PMID:27085672]
ChEMBL Inhibition of wild type B-Raf in human MIAPaCa2 cells assessed as reduction in ERK phosphorylation preincubated for 1 hr by Western blot method B 6.28 pEC50 529 nM EC50 Bioorg. Med. Chem. (2016) 24: 2215-2234 [PMID:27085672]
Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049]
ChEMBL Competitive binding affinity to CRAF in human A375 cells after 15 mins in presence of ATP analogue B 6.82 pIC50 150 nM IC50 J. Med. Chem. (2015) 58: 4165-4179 [PMID:25965804]
receptor interacting serine/threonine kinase 2/Serine/threonine-protein kinase RIPK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353]
ChEMBL Inhibition of human RIPK2 using MBP as substrate by [gamma33-ATP] based radiometric assay B 7.11 pIC50 77 nM IC50 J Med Chem (2020) 63: 1490-1510 [PMID:31622096]
transforming growth factor beta receptor 1/TGF-beta receptor type I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897]
ChEMBL Inhibition of Alk5 in TGF-beta-stimulated human HepG2 cells assessed as decrease in Smad2 phosphorylation treated for 45 mins prior to TGF-beta stimulation measured after 60 mins by odyssey blot scanner analysis B 5.43 pIC50 3700 nM IC50 ACS Med. Chem. Lett. (2013) 4: 358-362 [PMID:24900673]

ChEMBL data shown on this page come from version 28:

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]