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ChEMBL ligand: CHEMBL2403108 (Ceritinib, LDK378, NVP-LDK378-NX, Zykadia, LDK-378, NVP-LDK-378-NX) |
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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 | Binding affinity to wild-type human partial length ALK (I1088 to E1409 residues) expressed in mammalian expression system by KINOMEscan assay | B | 8.89 | pKd | 1.3 | nM | Kd | Eur J Med Chem (2018) 151: 304-314 [PMID:29627725] |
ChEMBL | Inhibition of ALK (unknown origin) | B | 5.43 | pKi | 3700 | nM | Ki | J Med Chem (2019) 62: 10005-10025 [PMID:31188592] |
ChEMBL | Inhibition of human N-terminal GST-tagged ALK G1202R mutant cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system after 1 hr by mobility shift assay | B | 4.04 | pIC50 | 91000 | nM | IC50 | Eur J Med Chem (2018) 158: 322-333 [PMID:30223120] |
ChEMBL | Inhibition of human N-terminal GST-tagged ALK L1196M mutant cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system after 1 hr by mobility shift assay | B | 4.46 | pIC50 | 35000 | nM | IC50 | Eur J Med Chem (2018) 158: 322-333 [PMID:30223120] |
ChEMBL | Inhibition of human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system after 1 hr by mobility shift assay | B | 5.54 | pIC50 | 2900 | nM | IC50 | Eur J Med Chem (2018) 158: 322-333 [PMID:30223120] |
ChEMBL | Inhibition of N-terminal GST-tagged human ALK G1202R mutant cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system using srctide as substrate incubated for 1 hr by mobility shift assay | B | 6.7 | pIC50 | 201 | nM | IC50 | Eur J Med Chem (2019) 171: 297-309 [PMID:30927566] |
ChEMBL | Inhibition of wild-type ALK (unknown origin) | B | 6.7 | pIC50 | 198 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1514-1517 [PMID:31005443] |
ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ALK (1058 to 1620 residues) cytoplasmic domain G1202R mutant using srctide as substrate incubated for 1 hr by mobility shift assay | B | 6.71 | pIC50 | 197 | nM | IC50 | Bioorg Med Chem (2019) 27: 115051-115051 [PMID:31492532] |
ChEMBL | Inhibition of ALK F1174L mutant (unknown origin) | B | 6.94 | pIC50 | 114.3 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1514-1517 [PMID:31005443] |
ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) G1202R mutant expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay | B | 7.04 | pIC50 | 91 | nM | IC50 | Eur J Med Chem (2018) 143: 123-136 [PMID:29174809] |
ChEMBL | Inhibition of ALK F1174L mutant auto-phosphorylation in human Kelly cells after 3 hrs by MSD assay | B | 7.1 | pIC50 | 79 | nM | IC50 | J Med Chem (2019) 62: 2618-2637 [PMID:30789735] |
ChEMBL | Inhibition of ALK L1196M mutant (unknown origin) using peptide as substrate after 60 mins by HTRF assay | B | 7.19 | pIC50 | 64 | nM | IC50 | Eur J Med Chem (2016) 123: 80-89 [PMID:27474925] |
ChEMBL | Inhibition of ALK L1196M mutant (unknown origin) | B | 7.32 | pIC50 | 47.65 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1514-1517 [PMID:31005443] |
ChEMBL | Inhibition of TEL-fused ALK (unknown origin) by cell-based assay | B | 7.39 | pIC50 | 40.7 | nM | IC50 | J. Med. Chem. (2013) 56: 5675-5690 [PMID:23742252] |
ChEMBL | Inhibition of ALK (unknown origin) transfected in mouse BA/F3 cells | B | 7.39 | pIC50 | 40.7 | nM | IC50 | J. Med. Chem. (2013) 56: 5673-5674 [PMID:23837797] |
ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) L1196M mutant expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay | B | 7.46 | pIC50 | 35 | nM | IC50 | Eur J Med Chem (2018) 143: 123-136 [PMID:29174809] |
ChEMBL | Inhibition of ALK L1196M mutant (unknown origin) after 30 mins by HTRF assay | B | 7.54 | pIC50 | 29 | nM | IC50 | Bioorg. Med. Chem. Lett. (2016) 26: 1720-1725 [PMID:26923695] |
ChEMBL | Inhibition of ALK L1196M mutant (unknown origin) by homogeneous time resolved fluorescence assay | B | 7.54 | pIC50 | 29 | nM | IC50 | Bioorg. Med. Chem. Lett. (2015) 25: 3992-3998 [PMID:26235945] |
ChEMBL | Inhibition of ALK L1196M mutant (unknown origin) using peptide as substrate measured after 30 mins by fluorescence assay | B | 7.54 | pIC50 | 29 | nM | IC50 | Eur J Med Chem (2017) 126: 536-549 [PMID:27915169] |
ChEMBL | Inhibition of ALK L1196M mutant (unknown origin) using TK as substrate after 30 mins by HTRF assay | B | 7.54 | pIC50 | 29 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2185-2191 [PMID:28385505] |
ChEMBL | Inhibition of NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay | B | 7.59 | pIC50 | 26 | nM | IC50 | J. Med. Chem. (2013) 56: 5675-5690 [PMID:23742252] |
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 | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
ChEMBL | Inhibition of wild type ALK (unknown origin) using TK as substrate after 30 mins by HTRF assay | B | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2185-2191 [PMID:28385505] |
ChEMBL | Inhibition of wild-type ALK (unknown origin) using peptide as substrate measured after 30 mins by fluorescence assay | B | 7.85 | pIC50 | 14 | nM | IC50 | Eur J Med Chem (2017) 126: 536-549 [PMID:27915169] |
ChEMBL | Inhibition of wild type ALK (unknown origin) after 30 mins by HTRF assay | B | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg. Med. Chem. Lett. (2016) 26: 1720-1725 [PMID:26923695] |
ChEMBL | Inhibition of wild type ALK (unknown origin) by homogeneous time resolved fluorescence assay | B | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg. Med. Chem. Lett. (2015) 25: 3992-3998 [PMID:26235945] |
ChEMBL | Inhibition of ALK G1202R mutant (unknown origin) using peptide as substrate measured after 30 mins by fluorescence assay | B | 7.89 | pIC50 | 13 | nM | IC50 | Eur J Med Chem (2017) 126: 536-549 [PMID:27915169] |
ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) S1206Y mutant expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay | B | 8.34 | pIC50 | 4.6 | nM | IC50 | Eur J Med Chem (2018) 143: 123-136 [PMID:29174809] |
ChEMBL | Inhibition of ALK (unknown origin) by TR-FRET assay | B | 8.4 | pIC50 | 3.94 | nM | IC50 | J Med Chem (2019) 62: 10927-10954 [PMID:31419130] |
ChEMBL | Inhibition of purified ALK (unknown origin) after 60 mins by ELISA kinase assay | B | 8.47 | pIC50 | 3.4 | nM | IC50 | Eur. J. Med. Chem. (2014) 86: 438-448 [PMID:25200979] |
ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) G1269A mutant expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay | B | 8.47 | pIC50 | 3.4 | nM | IC50 | Eur J Med Chem (2018) 143: 123-136 [PMID:29174809] |
ChEMBL | Inhibition of recombinant ALK (unknown origin) using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins by ELISA | B | 8.47 | pIC50 | 3.4 | nM | IC50 | Eur J Med Chem (2018) 144: 386-397 [PMID:29288940] |
ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ALK (1058 to 1620 residues) cytoplasmic domain L1196M mutant expressed in baculovirus expression system using srctide as substrate incubated for 1 hr by mobility shift assay | B | 8.51 | pIC50 | 3.1 | nM | IC50 | Bioorg Med Chem (2019) 27: 115051-115051 [PMID:31492532] |
ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay | B | 8.54 | pIC50 | 2.9 | nM | IC50 | Eur J Med Chem (2018) 143: 123-136 [PMID:29174809] |
ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) C1156Y mutant expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay | B | 8.54 | pIC50 | 2.9 | nM | IC50 | Eur J Med Chem (2018) 143: 123-136 [PMID:29174809] |
ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ALK (1058 to 1620 residues) cytoplasmic domain expressed in baculovirus expression system using srctide as substrate incubated for 1 hr by mobility shift assay | B | 8.57 | pIC50 | 2.7 | nM | IC50 | Bioorg Med Chem (2019) 27: 115051-115051 [PMID:31492532] |
ChEMBL | Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) T1151 insertion mutant expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay | B | 8.6 | pIC50 | 2.5 | nM | IC50 | Eur J Med Chem (2018) 143: 123-136 [PMID:29174809] |
ChEMBL | Inhibition of ALK (unknown origin) using peptide as substrate after 60 mins by HTRF assay | B | 8.64 | pIC50 | 2.3 | nM | IC50 | Eur J Med Chem (2016) 123: 80-89 [PMID:27474925] |
ChEMBL | Inhibition of N-terminal GST-tagged human ALK cytoplasmic domain (1058 to 1620 residues) expressed in Baculovirus expression system using srctide as substrate incubated for 1 hr by mobility shift assay | B | 8.64 | pIC50 | 2.3 | nM | IC50 | Eur J Med Chem (2019) 171: 297-309 [PMID:30927566] |
ChEMBL | Inhibition of EML4-fused ALK (unknown origin) by cell-based assay | B | 8.66 | pIC50 | 2.2 | nM | IC50 | J. Med. Chem. (2013) 56: 5675-5690 [PMID:23742252] |
ChEMBL | Inhibition of ALK C1156Y mutant (unknown origin) using peptide as substrate measured after 30 mins by fluorescence assay | B | 8.7 | pIC50 | 2 | nM | IC50 | Eur J Med Chem (2017) 126: 536-549 [PMID:27915169] |
ChEMBL | Inhibition of N-terminal GST-tagged human ALK L1196M mutant cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system using srctide as substrate incubated for 1 hr by mobility shift assay | B | 8.7 | pIC50 | 2 | nM | IC50 | Eur J Med Chem (2019) 171: 297-309 [PMID:30927566] |
ChEMBL | Inhibition of ALK F1174L mutant (unknown origin) using peptide as substrate measured after 30 mins by fluorescence assay | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Eur J Med Chem (2017) 126: 536-549 [PMID:27915169] |
ChEMBL | Inhibition of ALK G1269A mutant (unknown origin) using peptide as substrate measured after 30 mins by fluorescence assay | B | 8.85 | pIC50 | 1.4 | nM | IC50 | Eur J Med Chem (2017) 126: 536-549 [PMID:27915169] |
ChEMBL | Inhibition of ALK (unknown origin) after 60 mins | B | 9.7 | pIC50 | 0.2 | nM | IC50 | J. Med. Chem. (2013) 56: 5675-5690 [PMID:23742252] |
ChEMBL | Inhibition of ALK (unknown origin) | B | 9.7 | pIC50 | 0.2 | nM | IC50 | J. Med. Chem. (2013) 56: 5673-5674 [PMID:23837797] |
GtoPdb | - | - | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2013) 56: 5675-90 [PMID:23742252] |
ChEMBL | Inhibition of ALK L1152R mutant in human DFCI076 cells assessed as reduction in cell viability after 72 hrs by MTS assay | B | 5.46 | pEC50 | 3490 | nM | EC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
ChEMBL | Inhibition of ALK L1152R mutant in human DFCI076 cells assessed as reduction in cell viability after 72 hrs by MTS assay in presence of osimertinib | B | 5.49 | pEC50 | 3210 | nM | EC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
ChEMBL | Inhibition of CDK2 (unknown origin) after 60 mins | B | 5.4 | pIC50 | 3970 | nM | IC50 | J. Med. Chem. (2013) 56: 5675-5690 [PMID:23742252] |
cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802] | ||||||||
ChEMBL | Inhibition of CDK4 (unknown origin) after 60 mins | B | 5.33 | pIC50 | 4720 | nM | IC50 | J. Med. Chem. (2013) 56: 5675-5690 [PMID:23742252] |
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
ChEMBL | Inhibition of human N-terminal GST-tagged EGFR cytoplasmic domain (669 to 1210 residues) expressed in baculovirus expression system after 1 hr by mobility shift assay | B | 3 | pIC50 | >1000000 | nM | IC50 | Eur J Med Chem (2018) 158: 322-333 [PMID:30223120] |
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 | 5.67 | pIC50 | 2156 | nM | IC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
ChEMBL | Inhibition of recombinant human N-terminal GST-tagged EGFR cytoplasmic domain (669 to 1210 residues) expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2018) 143: 123-136 [PMID:29174809] |
ChEMBL | Inhibition of N-terminal GST-tagged human EGFR cytoplasmic domain (669 to 1210 residues) expressed in Baculovirus expression system using srctide as substrate incubated for 1 hr by mobility shift assay | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2019) 171: 297-309 [PMID:30927566] |
ChEMBL | Inhibition of recombinant human N-terminal GST-tagged EGFR (669 to 1210 residues) cytoplasmic domain expressed in baculovirus expression system using Srctide as substrate incubated for 1 hr by mobility shift assay | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem (2019) 27: 115051-115051 [PMID:31492532] |
ChEMBL | Inhibition of EGFR (unknown origin) using peptide as substrate after 60 mins by HTRF assay | B | 6 | pIC50 | >1000 | nM | IC50 | Eur J Med Chem (2016) 123: 80-89 [PMID:27474925] |
ChEMBL | Inhibition of EGFR (unknown origin) after 60 mins | B | 6.05 | pIC50 | 900 | nM | IC50 | J. Med. Chem. (2013) 56: 5675-5690 [PMID:23742252] |
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 | 7.55 | pIC50 | 28 | nM | IC50 | Eur J Med Chem (2017) 136: 497-510 [PMID:28528303] |
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 | 7.72 | pIC50 | 19 |