BDBM50436850 CERITINIB::CHEMBL2403108::LDK378::US10053458, Comparative Example 2::US10618884, Example 16::US9809572, Example 16

SMILES CC(C)Oc1cc(C2CCNCC2)c(C)cc1Nc1ncc(Cl)c(Nc2ccccc2S(=O)(=O)C(C)C)n1

InChI Key InChIKey=VERWOWGGCGHDQE-UHFFFAOYSA-N

Data  4 KI  174 IC50  1 Kd  11 EC50

PDB links: 1 PDB ID matches this monomer.

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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 190 hits for monomerid = 50436850   

TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 41nMAssay Description:Inhibition of ALK (unknown origin) transfected in mouse BA/F3 cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of ALK (unknown origin)More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 3.70E+3nMpH: 7.5Assay Description:Inhibitors (initial concentration 10 or 60 μM, three-fold serial dilutions) were incubated with IRE1α* in cleavage buffer (20 mM HEPES at p...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 3.40nMAssay Description:Inhibition of purified ALK (unknown origin) after 60 mins by ELISA kinase assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 14nMAssay Description:Inhibition of wild type ALK (unknown origin) by homogeneous time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 29nMAssay Description:Inhibition of ALK L1196M mutant (unknown origin) by homogeneous time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetInsulin receptor(Human)
Korea Research Institute of Chemical Technology

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 93nMAssay Description:Inhibition of insulin receptor (unknown origin) by homogeneous time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 14nMAssay Description:Inhibition of wild type ALK (unknown origin) after 30 mins by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 29nMAssay Description:Inhibition of ALK L1196M mutant (unknown origin) after 30 mins by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetHepatocyte growth factor receptor(Human)
Shenyang Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 1.00E+3nMAssay Description:Inhibition of c-Met (unknown origin) using peptide as substrate after 60 mins by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
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
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetProto-oncogene tyrosine-protein kinase ROS(Human)
Shenyang Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
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
In DepthDetails Article
PubMed
TargetEpidermal growth factor receptor(Human)
Shenyang Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 1.00E+3nMAssay Description:Inhibition of EGFR (unknown origin) using peptide as substrate after 60 mins by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetRho-associated protein kinase 2(Human)
Genomics Institute of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 1.27E+3nMAssay Description:Inhibition of ROCK2 (unknown origin) after 60 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTyrosine-protein kinase ABL1(Human)
Genomics Institute of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 1.25E+3nMAssay Description:Inhibition of ABL (unknown origin) after 60 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPlatelet-derived growth factor receptor alpha(Human)
Genomics Institute of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 1.14E+3nMAssay Description:Inhibition of PDGFRalpha (unknown origin) after 60 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Genomics Institute of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 610nMAssay Description:Inhibition of JAK2 (unknown origin) after 60 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Genomics Institute of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 400nMAssay Description:Inhibition of RET (unknown origin) after 60 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetReceptor-type tyrosine-protein kinase FLT3(Human)
Genomics Institute of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 60nMAssay Description:Inhibition of FLT3 (unknown origin) after 60 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTestis-specific serine/threonine-protein kinase 1(Human)
Genomics Institute of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 23nMAssay Description:Inhibition of STK22D (unknown origin) after 60 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetInsulin-like growth factor 1 receptor(Human)
Genomics Institute of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 8nMAssay Description:Inhibition of IGF1 receptor (unknown origin) after 60 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetInsulin receptor(Human)
Korea Research Institute of Chemical Technology

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 7nMAssay Description:Inhibition of insulin receptor (unknown origin) after 60 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of ALK (unknown origin) after 60 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 26nMAssay Description:Inhibition of NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase ZAP-70(Human)
Genomics Institute of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 9.70E+3nMAssay Description:Inhibition of ZAP70 (unknown origin) after 60 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTyrosine-protein kinase JAK3(Human)
Genomics Institute of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 7.92E+3nMAssay Description:Inhibition of JAK3 (unknown origin) after 60 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTyrosine-protein kinase JAK1(Human)
Genomics Institute of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 3.73E+3nMAssay Description:Inhibition of JAK1 (unknown origin) after 60 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTyrosine-protein kinase BTK(Human)
Genomics Institute of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 3.36E+3nMAssay Description:Inhibition of BTK (unknown origin) after 60 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHepatocyte growth factor receptor(Human)
Shenyang Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 3.17E+3nMAssay Description:Inhibition of cMET (unknown origin) after 60 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTyrosine-protein kinase SYK(Human)
Genomics Institute of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 3.05E+3nMAssay Description:Inhibition of SYK (unknown origin) after 60 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Human)
Genomics Institute of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 2.24E+3nMAssay Description:Inhibition of MKNK2 (unknown origin) after 60 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 2.20nMAssay Description:Inhibition of EML4-fused ALK (unknown origin) by cell-based assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Genomics Institute of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 2.30E+3nMAssay Description:Inhibition of TEL-fused RET (unknown origin) by cell-based assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
Genomics Institute of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 2.16E+3nMAssay Description:Inhibition of TEL-fused JAK2 (unknown origin) by cell-based assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBDNF/NT-3 growth factors receptor(Human)
Genomics Institute of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 1.83E+3nMAssay Description:Inhibition of TEL-fused TRKB (unknown origin) by cell-based assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHepatocyte growth factor receptor(Human)
Shenyang Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 1.34E+3nMAssay Description:Inhibition of TEL-fused MET (unknown origin) by cell-based assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetInsulin-like growth factor 1 receptor(Human)
Genomics Institute of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 410nMAssay Description:Inhibition of TEL-fused IGF1 receptor (unknown origin) by cell-based assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetInsulin receptor(Human)
Korea Research Institute of Chemical Technology

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 320nMAssay Description:Inhibition of TEL-fused insulin receptor (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetProto-oncogene tyrosine-protein kinase ROS(Human)
Shenyang Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 142nMAssay Description:Inhibition of TEL-fused ROS (unknown origin) by cell-based assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 41nMAssay Description:Inhibition of TEL-fused ALK (unknown origin) by cell-based assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetSerine/threonine-protein kinase PAK 2(Human)
Genomics Institute of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of PAK2 (unknown origin) after 60 minsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTranscription factor ETV6(Human)
Genomics Institute of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 3.25E+3nMAssay Description:Inhibition of wild-type TEL (unknown origin) by cell-based assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetReceptor-type tyrosine-protein kinase FLT3(Human)
Genomics Institute of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 3.14E+3nMAssay Description:Inhibition of TEL-fused FLT3 (unknown origin) by cell-based assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHigh affinity nerve growth factor receptor(Human)
Genomics Institute of The Novartis Research Foundation

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 2.73E+3nMAssay Description:Inhibition of TEL-fused TRKA (unknown origin) by cell-based assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
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
In DepthDetails
US Patent
PDB3D3D Structure (crystal)
TargetALK tyrosine kinase receptor [L1196M](Human)
Korea Research Institute of Chemical Technology

US Patent
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
In DepthDetails
US Patent
PDB3D3D Structure (crystal)
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 14nMAssay Description:Inhibition of wild-type ALK (unknown origin) using peptide as substrate measured after 30 mins by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 14nMAssay Description:Inhibition of wild type ALK (unknown origin) using TK as substrate after 30 mins by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetInsulin receptor(Human)
Korea Research Institute of Chemical Technology

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 24nMAssay Description:Inhibition of insulin receptor kinase (unknown origin) using TK as substrate after 30 mins by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetALK tyrosine kinase receptor(Human)
University of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
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
In DepthDetails
US Patent
PDB3D3D Structure (crystal)
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