BDBM50306682 (R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine::3-(2,6-dichloro-3-fluorobenzyloxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine::3-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)pyridin-2-amine::CHEMBL601719::CRIZOTINIB::PF-2341066::US10370379, Crizotinib::US10543199, Compound Crizotinib::US10780082, Compound Crizotinib::US11059827, Compound Crizotinib::US11517561, Compound Crizotinib::US9126941, PF-2341066::US9199944, Crizotinib::US9226923, Crizotinib

SMILES C[C@@H](Oc1cc(cnc1N)-c1cnn(c1)C1CCNCC1)c1c(Cl)ccc(F)c1Cl

InChI Key InChIKey=KTEIFNKAUNYNJU-GFCCVEGCSA-N

Data  13 KI  225 IC50  453 Kd  3 EC50  1 Koff

PDB links: 11 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 695 hits for monomerid = 50306682   

TargetProto-oncogene tyrosine-protein kinase ROS(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKi:  0.600nMAssay Description:Inhibition of wild type ROS1 (unknown origin)More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase ROS(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKi:  0.600nMAssay Description:Inhibition of ROS1 (unknown origin)More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKi:  0.740nMAssay Description:Inhibition of ALK (unknown origin)More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKi:  0.740nMAssay Description:Inhibition of wild type human recombinant ALK kinase domain (amino acids 1093 to 1141) expressed in baculovirus system using 5'FAM-KKSRGDYMTMQIG-CONH...More data for this Ligand-Target Pair
TargetHepatocyte growth factor receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKi:  2nMAssay Description:Binding affinity to human recombinant c-MET assessed as inhibition of autophosphorylation by continuous fluorometric assayMore data for this Ligand-Target Pair
TargetHepatocyte growth factor receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKi:  2nMAssay Description:Inhibition of c-Met (unknown origin)More data for this Ligand-Target Pair
TargetHepatocyte growth factor receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKi:  4nMAssay Description:Inhibition of c-Met (unknown origin)More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase ROS(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKi:  5.80nMAssay Description:Inhibition of ROS1 L2026M mutant (unknown origin)More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKi:  8.20nMAssay Description:Inhibition of L1196M mutant (unknown origin)More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKi:  8.20nMAssay Description:Inhibition of human recombinant ALK L1196M mutant kinase domain (amino acids 1093 to 1141) expressed in baculovirus system using 5'FAM-KKSRGDYMTMQIG-...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKi:  8.20nMAssay Description:Inhibition of ALK L1196M mutant (unknown origin)More data for this Ligand-Target Pair
TargetHepatocyte growth factor receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKi:  19nMAssay Description:Binding affinity to human recombinant c-MET assessed as inhibition of autophosphorylation by continuous fluorometric assayMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase ROS(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKi:  330nMAssay Description:Inhibition of ROS1 G2032R mutant (unknown origin)More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50: >2nMAssay Description:The compounds were evaluated in a transcriptional activation assay with hAR in a mammalian cell background (CV-1) as the primary in vitro assay. Rece...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  36nMT: 2°CAssay Description:In order to measure the inhibitory activity against ALK, a Grainer 96-well round type bottom plate was added with the compounds (2 μl) prepared ...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor [L1196M](Homo sapiens (Human))
Korea Research Institute Of Chemical Technology

US Patent
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  220nMT: 2°CAssay Description:In order to measure the inhibitory activity against ALK, a Grainer 96-well round type bottom plate was added with the compounds (2 μl) prepared ...More data for this Ligand-Target Pair
TargetIsoform 2 of Hepatocyte growth factor receptor (2)(Homo sapiens (Human))
Tianjin University Of Science And Technology

LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  13.7nMpH: 7.0 T: 2°CAssay Description:The c-Met kinase activity of five target compounds and three positive compounds were evaluated using standard Z-LYTE Assays (fluorescence resonance e...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  17.3nMpH: 7.5 T: 2°CAssay Description:The ALK kinase activity of five target compounds and three positive compounds were evaluated using standard homogeneous time-resolved fluorescence (H...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor [C1156Y](Homo sapiens (Human))
Tianjin University Of Science And Technology

LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  7.67nMpH: 7.5 T: 2°CAssay Description:The ALK kinase activity of five target compounds and three positive compounds were evaluated using standard homogeneous time-resolved fluorescence (H...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor [L1196M](Homo sapiens (Human))
Korea Research Institute Of Chemical Technology

US Patent
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  188nMpH: 7.5 T: 2°CAssay Description:The ALK kinase activity of five target compounds and three positive compounds were evaluated using standard homogeneous time-resolved fluorescence (H...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  2.10nMAssay Description:The inhibitory activities of compounds of Formula I were assay at Reaction Biology Corporation, One Great Valley Parkway, Malvern, Pa., USA. Human ...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor [C1156Y](Homo sapiens (Human))
Nanjing Allgen Pharma

US Patent
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50: <1.20nMAssay Description:The inhibitory activities of compounds of Formula I were assay at Reaction Biology Corporation, One Great Valley Parkway, Malvern, Pa., USA. Human ...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase receptor(Homo sapiens (Human))
Nanjing Allgen Pharma

US Patent
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  2.70nMAssay Description:The inhibitory activities of compounds of Formula I were assay at Reaction Biology Corporation, One Great Valley Parkway, Malvern, Pa., USA. Human ...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor [L1196M](Homo sapiens (Human))
Korea Research Institute Of Chemical Technology

US Patent
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  7.40nMAssay Description:The inhibitory activities of compounds of Formula I were assay at Reaction Biology Corporation, One Great Valley Parkway, Malvern, Pa., USA. Human ...More data for this Ligand-Target Pair
TargetTyrosine-protein kinase receptor(Homo sapiens (Human))
Nanjing Allgen Pharma

US Patent
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  2.90nMAssay Description:The inhibitory activities of compounds of Formula I were assay at Reaction Biology Corporation, One Great Valley Parkway, Malvern, Pa., USA. Human ...More data for this Ligand-Target Pair
TargetEphrin type-A receptor 2 [596-900](Homo sapiens (Human))
Technical University Of Munich

LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKd:  772nMAssay Description:Kinobeads competition assays were performed in 96-well format as previously described using mixed protein lysates of four cancer cell lines (K-562, M...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  5.5nMAssay Description:The inhibition of ALK tyrosine kinase activity can be demonstrated using known methods. For example, in one method, compounds can be tested for their...More data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor [L1196M](Homo sapiens (Human))
Korea Research Institute Of Chemical Technology

US Patent
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  55nMAssay Description:The inhibition of ALK tyrosine kinase activity can be demonstrated using known methods. For example, in one method, compounds can be tested for their...More data for this Ligand-Target Pair
TargetEpidermal growth factor receptor(Homo sapiens (Human))
Vichem Chemie Research

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50: >1.25E+4nMAssay Description:Inhibition of recombinant EGFR (unknown origin) using poly-GT peptide as substrate by Transcreener assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHepatocyte growth factor receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  2.40nMAssay Description:Inhibition of purified recombinant c-MET (unknown origin) after 60 mins by ELISAMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  28nMAssay Description:Inhibition of purified recombinant ALK (unknown origin) after 60 mins by ELISAMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  165nMAssay Description:Inhibition of human EML4-fused ALK F1174L mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISAMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  478nMAssay Description:Inhibition of human EML4-fused ALK C1156Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISAMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  605nMAssay Description:Inhibition of human EML4-fused ALK G1269A mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISAMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  626nMAssay Description:Inhibition of human EML4-fused ALK S1206Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISAMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  1.03E+3nMAssay Description:Inhibition of human EML4-fused ALK L1152R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISAMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  1.15E+3nMAssay Description:Inhibition of human EML4-fused ALK G1202R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISAMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  3.04E+3nMAssay Description:Inhibition of human EML4-fused ALK 1151Tins mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISAMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  80nMAssay Description:Inhibition of wild type human EML4-fused ALK expressed in mouse NIH-3T3 cells assessed as phosphorylated ALK level after 1 hr by sandwich ELISAMore data for this Ligand-Target Pair
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  843nMAssay Description:Inhibition of human EML4-fused ALK L1196M mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISAMore data for this Ligand-Target Pair
TargetInsulin receptor(Homo sapiens (Human))
St. Jude Children'S Research Hospital

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  650nMAssay Description:Inhibition of recombinant IRK using biotinylated-poly(GT) peptide as substrate after 60 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
Taibah University

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50:  600nMAssay Description:Inhibition of 6xHis-tagged NPM-ALK using biotinylated-poly(GT) peptide as substrate after 60 minsMore data for this Ligand-Target Pair
TargetNon-receptor tyrosine-protein kinase TYK2(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKd:  210nMAssay Description:Binding constant for TYK2(JH1domain-catalytic) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEphrin type-A receptor 1(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKd:  140nMAssay Description:Binding constant for EPHA1 kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMisshapen-like kinase 1(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKd:  4.40E+3nMAssay Description:Binding constant for MINK kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase MRCK gamma(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for DMPK2 kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(C420R) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase ABL1(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKd:  170nMAssay Description:Binding constant for ABL1(E255K)-phosphorylated kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargeteIF-2-alpha kinase GCN2(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for GCN2(Kin.Dom.2,S808G) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform(Homo sapiens (Human))
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataKd: >1.00E+4nMAssay Description:Binding constant for PIK3CA(E542K) kinase domainMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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