BDBM50436850 CERITINIB::CHEMBL2403108::LDK378::US10053458, Comparative Example 2::US10618884, Example 16::US12129258, Example Ceritinib::US9809572, Example 16
SMILES Cc1cc(c(cc1C2CCNCC2)OC(C)C)Nc3ncc(c(n3)Nc4ccccc4S(=O)(=O)C(C)C)Cl
InChI Key InChIKey=VERWOWGGCGHDQE-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 216 hits for monomerid = 50436850
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 0.200nMAssay Description:Inhibition of ALK (unknown origin)More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 0.200nMAssay Description:Inhibition of ALK (unknown origin) after 60 minsMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 0.25nMAssay Description:Inhibition of ALK L1196M mutant (unknown origin)More data for this Ligand-Target Pair
Affinity DataKi: 0.400nMAssay Description:Inhibition of ROS1 L2026M mutant (unknown origin)More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 0.610nMAssay Description:Inhibition of N-terminal GST tagged wild-type human ALK cytoplasmic domain (1058-1620 amino acids) expressed Sf9 cells pre-incubated for 30 mins befo...More data for this Ligand-Target Pair
Affinity DataKi: 0.700nMAssay Description:Inhibition of wild type ROS1 (unknown origin)More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 0.830nMAssay Description:Inhibition of wild type N-terminal GST tagged ALK L1196M mutant cytoplasmic domain (1058 to 1620 end residues) (unknown origin) expressed in Sf21 cel...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 1nMT: 2°CAssay Description:A proliferation inhibitory activity against the ALK of the compound represented by Chemical Formula 1 according to the present invention at an enzyme...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 1nMAssay Description:Inhibition of ALK (unknown origin) preincubated for 10 mins followed by addition of substrate and ATP for 25 mins by caliper EZ reader methodMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 1.10nMAssay Description:Inhibition of human ALK L1196M mutant expressed Sf9 cells pre-incubated for 30 mins before addition of Ulight-CKKSRGDYMTMQIG substrate and measured a...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 1.20nMAssay Description:Inhibition of wild type N-terminal GST tagged ALK cytoplasmic domain (1058 to 1620 end residues) (unknown origin) expressed in Sf21 cells incubated f...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataKd: 1.30nMAssay Description:Binding affinity to wild-type human partial length ALK (I1088 to E1409 residues) expressed in mammalian expression system by KINOMEscan assayMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 1.60nMAssay Description:Inhibition of human ALK S1206Y mutant expressed Sf9 cells pre-incubated for 30 mins before addition of Ulight-CKKSRGDYMTMQIG substrate and measured a...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 1.90nMAssay Description:Inhibition of human ALK G1269A mutant expressed Sf9 cells pre-incubated for 30 mins before addition of Ulight-CKKSRGDYMTMQIG substrate and measured a...More data for this Ligand-Target Pair
Affinity DataIC50: 2nMAssay Description:Inhibition of ROS1 (unknown origin) using peptide as substrate after 60 mins by HTRF assayMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 2nMAssay Description:Inhibition of N-terminal GST-tagged human ALK L1196M mutant cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system usi...More data for this Ligand-Target Pair
Affinity DataIC50: 2nMAssay Description:Inhibition of ROS1 (unknown origin) using peptide substrate incubated for 60 mins in presence of ATP by HTRF assayMore data for this Ligand-Target Pair
Affinity DataIC50: 2nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged ROS1 cytoplasmic domain (1883 to 2347 residues) expressed in baculovirus expression system usin...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 2.10nMAssay Description:Inhibition of crizotinib-resistant ALK G1269A mutant (unknown origin) using peptide substrate incubated for 30 mins in presence of ATP by fluorescenc...More data for this Ligand-Target Pair
Affinity DataIC50: 2.20nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged ROS1 (1883 to 2347 residues) expressed in baculovirus expression system using IRS1 as substrate...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 2.20nMAssay Description:Inhibition of EML4-fused ALK (unknown origin) by cell-based assayMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 2.30nMAssay Description:Inhibition of ALK (unknown origin) using peptide as substrate after 60 mins by HTRF assayMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 2.30nMAssay Description:Inhibition of N-terminal GST-tagged human ALK cytoplasmic domain (1058 to 1620 residues) expressed in Baculovirus expression system using srctide as ...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 2.40nMAssay Description:Inhibition of wild-type ALK (unknown origin) incubated for 1 hrMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 2.40nMAssay Description:Inhibition of crizotinib-resistant ALK F1174L mutant (unknown origin) using peptide substrate incubated for 30 mins in presence of ATP by fluorescenc...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 2.5nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) T1151 insertion mutant expressed in baculovirus ...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 2.60nMAssay Description:Inhibition of ALK (unknown origin) incubated for 1 hr and measured by mobility shift assayMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 2.70nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged ALK (1058 to 1620 residues) cytoplasmic domain expressed in baculovirus expression system using...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 2.90nMAssay Description:Inhibition of ALK (unknown origin) using peptide substrate incubated for 60 mins in presence of ATP by HTRF assayMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 2.90nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system using...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 2.90nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) C1156Y mutant expressed in baculovirus expressio...More data for this Ligand-Target Pair
Affinity DataIC50: 3.10nMAssay Description:Inhibition of N-terminal GST-tagged human ROS1 cytoplasmic domain (1883 to 2347 residues) expressed in Baculovirus expression system using IRS1 as su...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 3.10nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged ALK (1058 to 1620 residues) cytoplasmic domain L1196M mutant expressed in baculovirus expressio...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 3.10nMAssay Description:Inhibition of human ALK assessed as decreased enzymatic reactions measured after 1 hr by mobility shift assayMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 3.20nMAssay Description:Inhibition of human N-terminal GST-fused ALK cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus infected Sf21 insect cells using Src...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 3.20nMAssay Description:Inhibition of N-terminal GST-tagged human wild type ALK (1058 to 1620 residues) cytoplasmic domain expressed in baculovirus infected Sf21 cells incub...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 3.30nMAssay Description:Inhibition of ALK G1202R mutant (unknown origin)More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 3.40nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) G1269A mutant expressed in baculovirus expressio...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 3.40nMAssay Description:Inhibition of recombinant ALK (unknown origin) using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins by ELISAMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 3.40nMAssay Description:Inhibition of purified ALK (unknown origin) after 60 mins by ELISA kinase assayMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 3.5nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged ALK (1058 to 1620 residues) expressed in baculovirus expression system using Srctide as substra...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 3.5nMAssay Description:Inhibition of wild type ALK (unknown origin)More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 3.90nMAssay Description:Inhibition of ALK (unknown origin) by TR-FRET assayMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 4.20nMAssay Description:Inhibition of crizotinib-resistant ALK C1156Y mutant (unknown origin) using peptide substrate incubated for 30 mins in presence of ATP by fluorescenc...More data for this Ligand-Target Pair
Affinity DataIC50: 4.30nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged ROS (1883 to 2347 residues) cytoplasmic domain expressed in baculovirus expression system using...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 4.60nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) S1206Y mutant expressed in baculovirus expressio...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
University of Michigan Comprehensive Cancer Center
Curated by ChEMBL
Affinity DataIC50: 5nMAssay Description:The determination of IC50 of the inhibiting effect to kinase ALK 96-well plates was coated under 37° C. with coating buffer (125 ul/well) overnig...More data for this Ligand-Target Pair

3D Structure (crystal)