BDBM144315 Gilteritinib::US11512074, Example T-9::US8969336, 547::US8969336, 577

SMILES CCc1nc(C(N)=O)c(Nc2ccc(N3CCC(CC3)N3CCN(C)CC3)c(OC)c2)nc1NC1CCOCC1

InChI Key InChIKey=GYQYAJJFPNQOOW-UHFFFAOYSA-N

Data  5 KI  32 IC50

PDB links: 2 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 37 hits for monomerid = 144315   

TargetReceptor-type tyrosine-protein kinase FLT3(Homo sapiens (Human))
University Of South Australia

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataKi:  2nMAssay Description:Inhibition of FLT3 ITD mutant (unknown origin) using Glu/Tyr peptide substrate incubated for 120 mins measured after 40 mins incubation under dark by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor-type tyrosine-protein kinase FLT3(Homo sapiens (Human))
University Of South Australia

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataKi:  10nMAssay Description:Inhibition of wild type FLT3 (unknown origin) using Glu/Tyr peptide substrate incubated for 120 mins measured after 40 mins incubation under dark by ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase 2/G1/S-specific cyclin-E1(Homo sapiens (Human))
University Of South Australia

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataKi:  1.49E+3nMAssay Description:Inhibition of CDK2/cyclin E (unknown origin) using histone 1 protein substrate incubated for 120 mins measured after 40 mins incubation under dark by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCDK-activating kinase assembly factor MAT1/Cyclin-H/Cyclin-dependent kinase 7(Homo sapiens (Human))
University Of South Australia

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataKi: >5.00E+3nMAssay Description:Inhibition of CDK7/cyclin H/MAT1 (unknown origin) using HYSPTSPSYSPTSPSYSPTSPSKKKK-O substrate incubated for 120 mins measured after 40 mins incubati...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCyclin-dependent kinase/G2/mitotic-specific cyclin- 1(Homo sapiens (Human))
University Of South Australia

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataKi: >5.00E+3nMAssay Description:Inhibition of CDK1/cyclin B (unknown origin) using histone 1 protein substrate incubated for 120 mins measured after 40 mins incubation under dark by...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReplicase polyprotein 1ab(2019-nCoV)
Institut Pasteur Korea

LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  6.76E+3nMAssay Description:Ten-point DRCs were generated for each drug. Vero cells were seeded at 1.2 × 104 cells per well in DMEM, supplemented with 2% FBS and 1× ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor-type tyrosine-protein kinase FLT3(Homo sapiens (Human))
University Of South Australia

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  0.290nMAssay Description:Inhibition of N-terminal GST-tagged human FLT3 (564 to 993 residues) cytoplasmic domain expressed in baculovirus expression system by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase receptor UFO(Homo sapiens (Human))
Sichuan Academy Of Medical Science & Sichuan Provincial People'S Hospital

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  0.730nMAssay Description:Inhibition of N-terminal GST-tagged human AXL (464 to 885 residues) cytoplasmic domain expressed in baculovirus expression system by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTranscription factor ETV6/Tyrosine-protein kinase receptor UFO(Homo sapiens (Human))
Shanghai University

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  8.5nMAssay Description:Inhibition of TEL/AXL (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by SRB assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase receptor UFO(Homo sapiens (Human))
Sichuan Academy Of Medical Science & Sichuan Provincial People'S Hospital

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  11nMAssay Description:Inhibition of AXL (unknown origin) using poly (Glu, Tyr) as substrate after 60 mins by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor-type tyrosine-protein kinase FLT3(Homo sapiens (Human))
University Of South Australia

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  0.290nMAssay Description:Inhibition of FLT3 expressed in human SEMK2 cells assessed as reduction in FLT3 phosphorylation incubated for 1 hr by immunoblotting analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase receptor UFO(Homo sapiens (Human))
Sichuan Academy Of Medical Science & Sichuan Provincial People'S Hospital

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  4.60nMAssay Description:Inhibition of AXL (unknown origin) using poly [Glu, Tyr] 4:1 as substrate incubated for 60 mins in presence of ATP by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor-type tyrosine-protein kinase FLT3(Homo sapiens (Human))
University Of South Australia

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  1.10E+4nMAssay Description:Inhibition of FLT3 (unknown origin) using MBP as substrate incubated for 40 mins in presence of ATP by ADP-Glo assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase receptor UFO(Homo sapiens (Human))
Sichuan Academy Of Medical Science & Sichuan Provincial People'S Hospital

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  7.46nMAssay Description:The test compounds were dissolved in DMSO, and subjected to a 3-fold serial gradient dilution for 10 times. AXL kinase was transferred with different...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase receptor UFO(Homo sapiens (Human))
Sichuan Academy Of Medical Science & Sichuan Provincial People'S Hospital

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  7.35nMAssay Description:The test compounds were dissolved in DMSO, and subjected to a 3-fold serial gradient dilution for 10 times. AXL kinase was transferred with different...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase receptor UFO(Homo sapiens (Human))
Sichuan Academy Of Medical Science & Sichuan Provincial People'S Hospital

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  7.01nMAssay Description:The test compounds were dissolved in DMSO, and subjected to a 3-fold serial gradient dilution for 10 times. AXL kinase was transferred with different...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase receptor UFO(Homo sapiens (Human))
Sichuan Academy Of Medical Science & Sichuan Provincial People'S Hospital

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  6.62nMAssay Description:The test compounds were dissolved in DMSO, and subjected to a 3-fold serial gradient dilution for 10 times. AXL kinase was transferred with different...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase receptor UFO(Homo sapiens (Human))
Sichuan Academy Of Medical Science & Sichuan Provincial People'S Hospital

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  5.87nMAssay Description:The test compounds were dissolved in DMSO, and subjected to a 3-fold serial gradient dilution for 10 times. AXL kinase was transferred with different...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase receptor UFO(Homo sapiens (Human))
Sichuan Academy Of Medical Science & Sichuan Provincial People'S Hospital

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  5.33nMAssay Description:The test compounds were dissolved in DMSO, and subjected to a 3-fold serial gradient dilution for 10 times. AXL kinase was transferred with different...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase receptor UFO(Homo sapiens (Human))
Sichuan Academy Of Medical Science & Sichuan Provincial People'S Hospital

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  5.15nMAssay Description:The test compounds were dissolved in DMSO, and subjected to a 3-fold serial gradient dilution for 10 times. AXL kinase was transferred with different...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase receptor UFO(Homo sapiens (Human))
Sichuan Academy Of Medical Science & Sichuan Provincial People'S Hospital

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  6.24nMAssay Description:The test compounds were dissolved in DMSO, and subjected to a 3-fold serial gradient dilution for 10 times. AXL kinase was transferred with different...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase receptor UFO(Homo sapiens (Human))
Sichuan Academy Of Medical Science & Sichuan Provincial People'S Hospital

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  7.10nMAssay Description:The test compounds were dissolved in DMSO, and subjected to a 3-fold serial gradient dilution for 10 times. AXL kinase was transferred with different...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase receptor UFO(Homo sapiens (Human))
Sichuan Academy Of Medical Science & Sichuan Provincial People'S Hospital

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  6.5nMAssay Description:The test compounds were dissolved in DMSO, and subjected to a 3-fold serial gradient dilution for 10 times. AXL kinase was transferred with different...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetTyrosine-protein kinase receptor UFO(Homo sapiens (Human))
Sichuan Academy Of Medical Science & Sichuan Provincial People'S Hospital

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  0.730nMAssay Description:Inhibition of AXL (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetReceptor-type tyrosine-protein kinase FLT3(Homo sapiens (Human))
University Of South Australia

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  0.290nMAssay Description:Inhibition of Flt3 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetReceptor-type tyrosine-protein kinase FLT3(Homo sapiens (Human))
University Of South Australia

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  0.290nMAssay Description:Inhibition of FLT3 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetTyrosine-protein kinase receptor UFO(Homo sapiens (Human))
Sichuan Academy Of Medical Science & Sichuan Provincial People'S Hospital

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  0.730nMAssay Description:Inhibition of AXL (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  1.20nMAssay Description:Inhibition of ALK (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetReceptor-type tyrosine-protein kinase FLT3(Homo sapiens (Human))
University Of South Australia

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  0.290nMAssay Description:Inhibition of FLT3 (unknown origin) in presence of ATPMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetTyrosine-protein kinase receptor UFO(Homo sapiens (Human))
Sichuan Academy Of Medical Science & Sichuan Provincial People'S Hospital

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  0.730nMAssay Description:Inhibition of AXL (unknown origin) in presence of ATPMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetLeukocyte tyrosine kinase receptor(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  0.350nMAssay Description:Inhibition of LTK (unknown origin) in presence of ATPMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetTyrosine-protein kinase receptor UFO(Homo sapiens (Human))
Sichuan Academy Of Medical Science & Sichuan Provincial People'S Hospital

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50: <1nMAssay Description:Inhibition of AXL (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetReceptor-type tyrosine-protein kinase FLT3(Homo sapiens (Human))
University Of South Australia

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  0.410nMAssay Description:A partial protein of only a kinase domain of FLT3 protein was purchased from Carna Biosciences Inc., Japan, and tests were conducted as in Test Examp...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetProto-oncogene tyrosine-protein kinase ROS(Homo sapiens (Human))
Astellas Pharma

US Patent
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  1.90nMAssay Description:A partial protein of only a kinase domain of ROS protein was purchased from Carna Biosciences Inc., Japan, and tests were conducted as in Test Exampl...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetALK tyrosine kinase receptor(Homo sapiens (Human))
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  1.20nMAssay Description:Inhibition of ALK (unknown origin) in presence of ATPMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetTyrosine-protein kinase receptor(Homo sapiens (Human))
Astellas Pharma

US Patent
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  1.5nMAssay Description:A recombinant retrovirus was created from expression plasmid FLAG-EML4-ALKv1/pMX-iresCD8 in which cDNA for EMLA-ALK fusion protein v1 was integrated,...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Homo sapiens (Human))
Astellas Pharma

US Patent
LigandPNGBDBM144315(Gilteritinib | US11512074, Example T-9 | US8969336...)
Affinity DataIC50:  3.40nMAssay Description:A partial protein of only a kinase domain of RET protein was purchased from Carna Biosciences Inc., Japan. The phosphorylation activity toward a pept...More data for this Ligand-Target Pair
In DepthDetails US Patent