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ChEMBL ligand: CHEMBL1229592 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73] | ||||||||
ChEMBL | Inhibition of GST-tagged human ALK cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system using Poly G:T (4:1) as substrate after 30 mins by Z-LYTE assay | B | 6 | pIC50 | 990 | nM | IC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
cathepsin C/Dipeptidyl peptidase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2252] [GtoPdb: 2344] [UniProtKB: P53634] | ||||||||
ChEMBL | Inhibition of CatL-activated recombinant human C-terminal His10-tagged cathepsin C (25 to 463 residues) expressed in mouse myeloma cells using Gly-Phe-AFC as substrate preincubated for 3 hrs followed by substrate addition and measured after 60 mins | B | 5.68 | pIC50 | 2100 | nM | IC50 | J Med Chem (2019) 62: 5901-5919 [PMID:31145622] |
ChEMBL | Inhibition of cathepsin C (unknown origin) | B | 5.68 | pIC50 | 2100 | nM | IC50 | J Med Chem (2019) 62: 5901-5919 [PMID:31145622] |
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
ChEMBL | Binding affinity to recombinant EGFR L858R/T90M mutant | B | 6.89 | pKd | 130 | nM | Kd | J Med Chem (2012) 55: 6243-6262 [PMID:22621397] |
ChEMBL | Binding affinity to EGFR | B | 7.34 | pKd | 46 | nM | Kd | J Med Chem (2012) 55: 2711-2723 [PMID:22339342] |
GtoPdb | - | - | 7.34 | pKd | 46 | nM | Kd | Nature (2009) 462: 1070-4 [PMID:20033049] |
ChEMBL | Binding affinity to EGFR L858R mutant | B | 7.54 | pKd | 29 | nM | Kd | J Med Chem (2012) 55: 2711-2723 [PMID:22339342] |
ChEMBL | Binding affinity to partial length human EGFR L858R/T790M double mutant expressed in mammalian system by KINOMEscan assay | B | 9.52 | pKd | 0.3 | nM | Kd | J Med Chem (2016) 59: 6580-6594 [PMID:26882288] |
ChEMBL | Inhibition of EGFR in human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay | B | 4.74 | pIC50 | 18210 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4832-4837 [PMID:28974338] |
ChEMBL | Inhibition of EGFR E746_A750 deletion/T790M mutant in human growth-resistant PC9 cells assessed as reduction in cell viability after 72 hrs by MTT assay | B | 5.07 | pIC50 | 8600 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4832-4837 [PMID:28974338] |
ChEMBL | Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in baculovirus expression system by ELISA | B | 5.15 | pIC50 | 7000 | nM | IC50 | Eur J Med Chem (2017) 140: 510-527 [PMID:28987609] |
ChEMBL | Inhibition of recombinant human N-terminally GST-tagged EGFR L858R/T790M/C797S triple mutant expressed in baculovirus in Sf9 insect cells preincubated for 20 mins followed by addition of [33P]-ATP measured after 2 hrs by filter-binding method | B | 5.69 | pIC50 | 2050 | nM | IC50 | J Med Chem (2017) 60: 4636-4656 [PMID:28482151] |
ChEMBL | Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay | B | 5.93 | pIC50 | 1180 | nM | IC50 | J Med Chem (2013) 56: 7025-7048 [PMID:23930994] |
ChEMBL | Inhibition of wild-type EGFR phosphorylation in human A431 cells preincubated for 1 hr followed by EGF stimulation measured after 45 mins by ELISA | B | 6.15 | pIC50 | 710 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 1257-1261 [PMID:29534926] |
ChEMBL | Inhibition of wild type GST-tagged human EGFR cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using Poly G:T (4:1) as substrate after 30 mins by Z-LYTE assay | B | 6.92 | pIC50 | 120 | nM | IC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
ChEMBL | Inhibition of EGFR E746_A750 deletion mutant in human PC9 cells assessed as reduction in cell viability after 72 hrs by MTT assay | B | 6.96 | pIC50 | 110 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4832-4837 [PMID:28974338] |
ChEMBL | Inhibition of wild type recombinant human EGFR preincubated for 10 mins followed by FAM-labeled peptide/ATP addition measured after 1 hr by mobility shift assay | B | 7.1 | pIC50 | 79 | nM | IC50 | Eur J Med Chem (2015) 104: 115-126 [PMID:26451770] |
ChEMBL | Inhibition of EGFR L858R/T790M mutant phosphorylation in human NCI-H1975 cells after 1 hr by ELISA | B | 7.34 | pIC50 | 46 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 1257-1261 [PMID:29534926] |
ChEMBL | Inhibition of wild-type EGFR (unknown origin) expressed in baculovirus expression system after 1 hr by ELISA | B | 7.51 | pIC50 | 31.1 | nM | IC50 | Bioorg Med Chem (2016) 24: 2673-2680 [PMID:27131639] |
ChEMBL | Inhibition of human recombinant EGFR T790M/L858R double mutant preincubated for 10 mins followed by FAM-labeled peptide/ATP addition measured after 1 hr by mobility shift assay | B | 7.51 | pIC50 | 31 | nM | IC50 | Eur J Med Chem (2015) 104: 115-126 [PMID:26451770] |
ChEMBL | Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay | B | 7.64 | pIC50 | 23 | nM | IC50 | J Med Chem (2013) 56: 7025-7048 [PMID:23930994] |
ChEMBL | Inhibition of recombinant human GST-tagged wild-type EGFR cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 1257-1261 [PMID:29534926] |
ChEMBL | Inhibition of wild type N-terminal His6-tagged human EGFR kinase domain (702 to 1016 residues) expressed in Sf9 cells pre-incubated for 30 mins before ATP and substrate addition by homogeneous time-resolved FRET assay | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem (2015) 23: 2767-2780 [PMID:25975640] |
ChEMBL | Inhibition of wild type EGFR (unknown origin) expressed in Sf9 cells pre-incubated for 30 mins before substrate and ATP addition by homogeneous time-resolved FRET assay | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2015) 58: 6844-6863 [PMID:26275028] |
ChEMBL | Inhibition of EGFR T790M/L858R mutant (unknown origin) expressed in baculovirus expression system after 1 hr by ELISA | B | 8.01 | pIC50 | 9.7 | nM | IC50 | Bioorg Med Chem (2016) 24: 2673-2680 [PMID:27131639] |
ChEMBL | Inhibition of EGFR kinase L858R mutant (unknown origin) after 1.5 hrs by FRET-based Z'-Lyte assay | B | 8.09 | pIC50 | 8.13 | nM | IC50 | Medchemcomm (2012) 3: 1155-1159 |
ChEMBL | Inhibition of wild type EGFR kinase (unknown origin) after 1.5 hrs by FRET-based Z'-Lyte assay | B | 8.19 | pIC50 | 6.47 | nM | IC50 | Medchemcomm (2012) 3: 1155-1159 |
ChEMBL | Inhibition of EGFR L858R/T790M mutant (unknown origin) using Poly(Glu,Tyr)4:1 as substrate incubated for 1 hr by ELISA | B | 8.19 | pIC50 | 6.4 | nM | IC50 | Medchemcomm (2015) 6: 1693-1697 |
ChEMBL | Inhibition of EGFR after 1.5 hr by FRET assay | B | 8.21 | pIC50 | 6.18 | nM | IC50 | J Med Chem (2012) 55: 2711-2723 [PMID:22339342] |
ChEMBL | Inhibition of EGFR L861Q mutant after 1.5 hr by FRET assay | B | 8.21 | pIC50 | 6.13 | nM | IC50 | J Med Chem (2012) 55: 2711-2723 [PMID:22339342] |
ChEMBL | Inhibition of EGFR L858R mutant (unknown origin) after 1.5 hrs by FRET-based Z'Lyte assay | B | 8.27 | pIC50 | 5.4 | nM | IC50 | J Med Chem (2013) 56: 4738-4748 [PMID:23668441] |
ChEMBL | Inhibition of EGFR L858R mutant (unknown origin) using Tyr 4 peptide as substrate after 1.5 hrs by FRET based Z'-lyte assay | B | 8.27 | pIC50 | 5.4 | nM | IC50 | Eur J Med Chem (2013) 66: 82-90 [PMID:23792318] |
ChEMBL | Inhibition of EGFR L858R mutant after 1.5 hr by FRET assay | B | 8.27 | pIC50 | 5.37 | nM | IC50 | J Med Chem (2012) 55: 2711-2723 [PMID:22339342] |
ChEMBL | Inhibition of GST-tagged human EGFR T790M mutant cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using Poly G:T (4:1) as substrate after 30 mins by Z-LYTE assay | B | 8.3 | pIC50 | 5 | nM | IC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
ChEMBL | Inhibition of EGFR L858R mutant (unknown origin) after 1.5 hr by FRET-based Z-lyte assay | B | 8.32 | pIC50 | 4.8 | nM | IC50 | Eur J Med Chem (2014) 77: 75-83 [PMID:24607591] |
ChEMBL | Inhibition of N-terminal GST-tagged human recombinant EGFR L858R mutant (668 to 1210 residues) expressed in baculovirus expression system by Z'-LYTE kinase assay | B | 8.33 | pIC50 | 4.64 | nM | IC50 | Eur J Med Chem (2021) 211: 113022-113022 [PMID:33239261] |
ChEMBL | Inhibition of N-terminal GST-tagged human recombinant EGFR cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system by Z'-LYTE kinase assay | B | 8.34 | pIC50 | 4.59 | nM | IC50 | Eur J Med Chem (2021) 211: 113022-113022 [PMID:33239261] |
ChEMBL | Inhibition of EGFR (unknown origin) after 1.5 hr by FRET-based Z-lyte assay | B | 8.36 | pIC50 | 4.4 | nM | IC50 | Eur J Med Chem (2014) 77: 75-83 [PMID:24607591] |
ChEMBL | Inhibition of EGFR kinase L861Q mutant (unknown origin) after 1.5 hrs by FRET-based Z'-Lyte assay | B | 8.37 | pIC50 | 4.25 | nM | IC50 | Medchemcomm (2012) 3: 1155-1159 |
ChEMBL | Inhibition of GST-tagged human EGFR T790M/L858R double mutant cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using Poly G:T (4:1) as substrate after 30 mins by Z-LYTE assay | B | 8.4 | pIC50 | 4 | nM | IC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
ChEMBL | Inhibition of EGFR L858R mutant (unknown origin) using Tyr 4 peptide as substrate after 1.5 hrs by FRET-based Z'-LYTE assay | B | 8.42 | pIC50 | 3.82 | nM | IC50 | J Med Chem (2013) 56: 7821-7837 [PMID:24053674] |
ChEMBL | Inhibition of EGFR T790M mutant after 1.5 hr by FRET assay | B | 8.42 | pIC50 | 3.77 | nM | IC50 | J Med Chem (2012) 55: 2711-2723 [PMID:22339342] |
ChEMBL | Inhibition of wild type EGFR (unknown origin) using Tyr 4 peptide as substrate after 1.5 hrs by FRET based Z'-lyte assay | B | 8.49 | pIC50 | 3.2 | nM | IC50 | Eur J Med Chem (2013) 66: 82-90 [PMID:23792318] |
ChEMBL | Inhibition of wild type EGFR (unknown origin) after 1.5 hrs by FRET-based Z'Lyte assay | B | 8.49 | pIC50 | 3.2 | nM | IC50 | J Med Chem (2013) 56: 4738-4748 [PMID:23668441] |
ChEMBL | Inhibition of recombinant human GST-tagged EGFR L858R/T790M mutant cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 1257-1261 [PMID:29534926] |
ChEMBL | Inhibition of N-terminal GST-tagged human recombinant EGFR L861Q mutant (668 to 1210 residues) expressed in baculovirus expression system by Z'-LYTE kinase assay | B | 8.54 | pIC50 | 2.86 | nM | IC50 | Eur J Med Chem (2021) 211: 113022-113022 [PMID:33239261] |
ChEMBL | Inhibition of EGFR kinase T790M mutant (unknown origin) after 1.5 hrs by FRET-based Z'-Lyte assay | B | 8.61 | pIC50 | 2.47 | nM | IC50 | Medchemcomm (2012) 3: 1155-1159 |
ChEMBL | Inhibition of wild type EGFR (unknown origin) using Tyr 4 peptide as substrate after 1.5 hrs by FRET-based Z'-LYTE assay | B | 8.67 | pIC50 | 2.16 | nM | IC50 | J Med Chem (2013) 56: 7821-7837 [PMID:24053674] |
ChEMBL | Inhibition of N-terminal GST-tagged human recombinant EGFR T790M mutant (668 to 1210 residues) expressed in baculovirus expression system by Z'-LYTE kinase assay | B | 8.7 | pIC50 | 1.98 | nM | IC50 | Eur J Med Chem (2021) 211: 113022-113022 [PMID:33239261] |
ChEMBL | Inhibition of EGFR L858R/T790M mutant after 1.5 hr by FRET assay | B | 8.73 | pIC50 | 1.88 | nM | IC50 | J Med Chem (2012) 55: 2711-2723 [PMID:22339342] |
ChEMBL | Inhibition of EGFR kinase L858R/T790M double mutant (unknown origin) after 1.5 hrs by FRET-based Z'-Lyte assay | B | 8.74 | pIC50 | 1.82 | nM | IC50 | Medchemcomm (2012) 3: 1155-1159 |
ChEMBL | Inhibition of EGFR (unknown origin) using biotin-labelled peptide as substrate preincubated for 2 hrs followed by substrate addition and measured after 30 mins by HTRF FRET assay | B | 8.77 | pIC50 | 1.7 | nM | IC50 | J Med Chem (2019) 62: 5901-5919 [PMID:31145622] |
ChEMBL | Inhibition of EGFR L858R mutant (unknown origin) | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2017) 60: 4636-4656 [PMID:28482151] |
ChEMBL | Inhibition of human N-terminal GST-fused EGFR T790M/L858R double mutant (669 to 1210 residues) expressed in baculovirus using TK-substrate-biotin preincubated for 30 mins followed by substrate addition measured after 20 mins by HTFR assay | B | 9 | pIC50 | <1 | nM | IC50 | J Med Chem (2017) 60: 5613-5637 [PMID:28603991] |
ChEMBL | Inhibition of human recombinant GST-tagged EGFR L858R mutant expressed in baculovirus expression system preincubated for 30 mins followed by ATP and TK-substrate addition measured after 15 mins by HTRF assay | B | 9 | pIC50 | <1 | nM | IC50 | J Med Chem (2017) 60: 7725-7744 [PMID:28853575] |
ChEMBL | Inhibition of recombinant human GST-tagged EGFR L858R/T790M double mutant expressed in baculovirus expression system preincubated for 30 mins followed by ATP and TK-substrate addition measured after 20 mins by HTRF assay | B | 9 | pIC50 | <1 | nM | IC50 | J Med Chem (2017) 60: 7725-7744 [PMID:28853575] |
ChEMBL | Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay | B | 9 | pIC50 | <1 | nM | IC50 | J Med Chem (2015) 58: 6844-6863 [PMID:26275028] |
ChEMBL | Inhibition of EGFR L858R mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay | B | 9 | pIC50 | <1 | nM | IC50 | J Med Chem (2015) 58: 6844-6863 [PMID:26275028] |
ChEMBL | Inhibition of human N-terminal GST-fused EGFR L858R mutant (669 to 1210 residues) expressed in baculovirus using TK-substrate-biotin preincubated for 30 mins followed by substrate addition measured after 15 mins by HTFR assay | B | 9 | pIC50 | <1 | nM | IC50 | J Med Chem (2017) 60: 5613-5637 [PMID:28603991] |
ChEMBL | Inhibition of EGFR L858R/T90M double mutant (unknown origin) after 1.5 hrs by FRET-based Z'Lyte assay | B | 9.1 | pIC50 | 0.8 | nM | IC50 | J Med Chem (2013) 56: 4738-4748 [PMID:23668441] |
ChEMBL | Inhibition of EGFR L858R/T790M mutant (unknown origin) using Tyr 4 peptide as substrate after 1.5 hrs by FRET based Z'-lyte assay | B | 9.1 | pIC50 | 0.8 | nM | IC50 | Eur J Med Chem (2013) 66: 82-90 [PMID:23792318] |
ChEMBL | Inhibition of recombinant human N-terminal GST tagged EGFR L858R mutant (669 to 1210 residues) expressed in insect expression system using peptide as substrate incubated for 2 hrs followed by substrate addition and measured after 30 mins by TR-FRET assay | B | 9.1 | pIC50 | 0.8 | nM | IC50 | Bioorg Med Chem (2018) 26: 1740-1750 [PMID:29523467] |
ChEMBL | Inhibition of EGFR L858R/T790M mutant (unknown origin) after 1.5 hr by FRET-based Z-lyte assay | B | 9.15 | pIC50 | 0.7 | nM | IC50 | Eur J Med Chem (2014) 77: 75-83 [PMID:24607591] |
ChEMBL | Inhibition of EGFR T790M/L858R double mutant (unknown origin) using Tyr 4 peptide as substrate after 1.5 hrs by FRET-based Z'-LYTE assay | B | 9.18 | pIC50 | 0.66 | nM | IC50 | J Med Chem (2013) 56: 7821-7837 [PMID:24053674] |
ChEMBL | Inhibition of EGFR L858R/T790M double mutant (unknown origin) | B | 9.3 | pIC50 | <0.5 | nM | IC50 | J Med Chem (2017) 60: 4636-4656 [PMID:28482151] |
ChEMBL | Inhibition of GST-tagged human recombinant EGFR catalytic domain (668 to 1210 amino acids) L858R mutant expressed in Sf9 cells pre-incubated for 30 mins before ATP and substrate addition by homogeneous time-resolved FRET assay | B | 9.38 | pIC50 | 0.42 | nM | IC50 | Bioorg Med Chem (2015) 23: 2767-2780 [PMID:25975640] |
ChEMBL | Inhibition of GST-tagged human recombinant EGFR catalytic domain (668 to 1210 amino acids) T790M/L858R mutant expressed in Sf9 cells pre-incubated for 30 mins before ATP and substrate addition by homogeneous time-resolved FRET assay | B | 9.72 | pIC50 | 0.19 | nM | IC50 | Bioorg Med Chem (2015) 23: 2767-2780 [PMID:25975640] |
ChEMBL | Inhibition of recombinant human N-terminal GST tagged EGFR L858R/T790M double mutant (669 to 1210 residues) expressed in insect expression system using peptide as substrate incubated for 2 hrs followed by substrate addition and measured after 30 mins by TR-FRET assay | B | 10.4 | pIC50 | 0.04 | nM | IC50 | Bioorg Med Chem (2018) 26: 1740-1750 [PMID:29523467] |
ChEMBL | Inhibition of wild type EGFR (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay | B | 6 | pEC50 | 989 | nM | EC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
ChEMBL | Inhibition of EGFR exon19 deletion mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay | B | 7.17 | pEC50 | 68 | nM | EC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
ChEMBL | Inhibition of EGFR T790M/L858R double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay | B | 7.51 | pEC50 | 31 | nM | EC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
ChEMBL | Inhibition of EGFR T790M exon19 deletion double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay | B | 7.57 | pEC50 | 27 | nM | EC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
ChEMBL | Inhibition of EGFR L858R mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay | B | 7.59 | pEC50 | 26 | nM | EC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
NUAK family kinase 1/NUAK family SNF1-like kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5784] [GtoPdb: 2129] [UniProtKB: O60285] | ||||||||
GtoPdb | - | - | 7.04 | pKd | 91 | nM | Kd | Nature (2009) 462: 1070-4 [PMID:20033049] |
ChEMBL | Inhibition of N-terminal GST-tagged wild type human NUAK1 expressed in Escherichia coli DH5alpha incubated for 30 mins in presence of gamma-[32P]ATP by cerenkov counting analysis | B | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (2021) 64: 2-25 [PMID:33356242] |
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3099] [GtoPdb: 1923] [UniProtKB: P00520] | ||||||||
ChEMBL | Inhibition of ABL T315I mutant in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTT assay | B | 4.79 | pIC50 | 16280 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4832-4837 [PMID:28974338] |
ChEMBL | Inhibition of ABL in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTT assay | B | 5.01 | pIC50 | 9690 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4832-4837 [PMID:28974338] |
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] | ||||||||
ChEMBL | Binding affinity to JAK3 (unknown origin) | B | 6.82 | pKd | 150 | nM | Kd | J Med Chem (2015) 58: 6589-6606 [PMID:26258521] |
erb-b2 receptor tyrosine kinase 4 in Human [GtoPdb: 1799] [UniProtKB: Q15303] | ||||||||
GtoPdb | - | - | 7.55 | pKd | 28 | nM | Kd | Nature (2009) 462: 1070-4 [PMID:20033049] |
BLK proto-oncogene, Src family tyrosine kinase in Human [GtoPdb: 1940] [UniProtKB: P51451] | ||||||||
GtoPdb | - | - | 6.7 | pKd | 200 | nM | Kd | Nature (2009) 462: 1070-4 [PMID:20033049] |
Bruton tyrosine kinase in Human [GtoPdb: 1948] [UniProtKB: Q06187] | ||||||||
GtoPdb | - | - | 7.37 | pKd | 43 | nM | Kd | Nature (2009) 462: 1070-4 [PMID:20033049] |
IL2 inducible T cell kinase in Human [GtoPdb: 2046] [UniProtKB: Q08881] | ||||||||
GtoPdb | - | - | 7.37 | pKd | 43 | nM | Kd | Nature (2009) 462: 1070-4 [PMID:20033049] |
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]