BDBM296429 US10112942, Example 163::US10112942, Example 166::US10112942, Example 183::US10137124, Example 163::US10555944, Example 163::US10953005, Example 163::US12338253, Compound Selpercatinib(LOXO-292)::US20230322769, Compound Selpercatinib::US20240174674, Compound Selpercatinib::US20250268897, Compound LOXO-292
SMILES COc1ccc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OCC(C)(C)O)cn3ncc(C#N)c23)cn1
InChI Key InChIKey=XIIOFHFUYBLOLW-UHFFFAOYSA-N
Data 46 IC50
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 46 hits for monomerid = 296429
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affinity DataIC50: 0.100nMAssay Description:Inhibition of RET V804L mutant (unknown origin) by FRET-based ZLyte kinase assayMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affinity DataIC50: 0.177nMAssay Description:Inhibition of RET (unknown origin) preincubated for 10 mins followed by substrate/ATP addition measured after 30 mins by HTRF assayMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affinity DataIC50: 0.300nMAssay Description:Inhibition of RET M918T mutant (unknown origin) by FRET-based ZLyte kinase assayMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affinity DataIC50: 0.400nMAssay Description:Inhibition of wildtype RET (unknown origin) incubated for 120 mins by Perkin Elmer electrophoretic mobility shift platform methodMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affinity DataIC50: 0.400nMAssay Description:Inhibition of human wild type RETMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affinity DataIC50: 0.420nMAssay Description:Inhibition of recombinant RET V804L (unknown origin) incubated for 120 mins by Perkin Elmer electrophoretic mobility shift platform methodMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affinity DataIC50: 0.420nMAssay Description:Inhibition of human RET V804L mutantMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affinity DataIC50: 0.700nMAssay Description:Inhibition of recombinant RET M918T (unknown origin) incubated for 120 mins by Perkin Elmer electrophoretic mobility shift platform methodMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affinity DataIC50: 0.800nMAssay Description:Inhibition of human RET V804M mutantMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affinity DataIC50: 1.20nMAssay Description:Inhibition of GST-3C fused human RET (705 to 1013 residues) expressed in sf9 baculovirus expression system using 5-FAM- peptide as substrate preincub...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affinity DataIC50: 1.98nMAssay Description:The activity assay method for the above kinases was established by homogeneous time-resolved fluorescence (HTRF), and the inhibitory activity of the ...More data for this Ligand-Target Pair
TargetCoiled-coil domain-containing protein 6/Proto-oncogene tyrosine-protein kinase receptor Ret(Human)
Jiangsu Chia Tai Fenghai Pharmaceutical
US Patent
Jiangsu Chia Tai Fenghai Pharmaceutical
US Patent
Affinity DataIC50: 2.07nMAssay Description:The activity assay method for the above kinases was established by homogeneous time-resolved fluorescence (HTRF), and the inhibitory activity of the ...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affinity DataIC50: 2.10nMAssay Description:Inhibition of RET V804M mutant (unknown origin) by FRET-based ZLyte kinase assayMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [M918T](Human)
Jiangsu Chia Tai Fenghai Pharmaceutical
US Patent
Jiangsu Chia Tai Fenghai Pharmaceutical
US Patent
Affinity DataIC50: 2.17nMAssay Description:The activity assay method for the above kinases was established by homogeneous time-resolved fluorescence (HTRF), and the inhibitory activity of the ...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affinity DataIC50: 2.30nMAssay Description:Inhibition of wildtype RET (unknown origin) in presence of ATP by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affinity DataIC50: 2.80nMAssay Description:Inhibition of wild type rearranged during transfection kinase (unknown origin) preincubated for 1 hr followed by addition of development agent incuba...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affinity DataIC50: 3.60nMAssay Description:Inhibition of wild type RET (unknown origin) by FRET-based ZLyte kinase assayMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [V804M](Human)
Jiangsu Chia Tai Fenghai Pharmaceutical
US Patent
Jiangsu Chia Tai Fenghai Pharmaceutical
US Patent
Affinity DataIC50: 5.09nMAssay Description:The activity assay method for the above kinases was established by homogeneous time-resolved fluorescence (HTRF), and the inhibitory activity of the ...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [G810S](Human)
Sichuan Kelun-Biotech Biopharmaceutical Co.
US Patent
Sichuan Kelun-Biotech Biopharmaceutical Co.
US Patent
Affinity DataIC50: 5.66nMAssay Description:The three drug-resistant mutant RET enzymes were each pre-incubated with different concentrations of test compounds (in the inhibition rate test of t...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affinity DataIC50: 14nMAssay Description:Compounds of Formula I were screened for their ability to inhibit wildtype and V804M mutant RET kinase using CisBio's HTRF KinEASE -TK assay tech...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affinity DataIC50: 14nMpH: 7.4Assay Description:Compounds of Formula I were screened for their ability to inhibit wildtype and V804M mutant RET kinase using CisBio's HTRF KinEASE -TK assay tech...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affinity DataIC50: 14nMAssay Description:RET: Compounds of Formula I were screened for their ability to inhibit wildtype and V804M mutant RET kinase using CisBio's HTRF KinEASE -TK assay...More data for this Ligand-Target Pair
Affinity DataIC50: 14nMAssay Description:Compounds of Formula I were screened for their ability to inhibit wildtype and V804M mutant RET kinase using CisBio's HTRF KinEASE-TK assay techn...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affinity DataIC50: 15.1nMpH: 7.4Assay Description:Compounds of Formula I were screened for their ability to inhibit wildtype and V804M mutant RET kinase using CisBio's HTRF KinEASE -TK assay tech...More data for this Ligand-Target Pair
Affinity DataIC50: 24.1nMAssay Description:Compounds of Formula I were screened for their ability to inhibit wildtype and V804M mutant RET kinase using CisBio's HTRF KinEASE-TK assay techn...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [V804M](Human)
Jiangsu Chia Tai Fenghai Pharmaceutical
US Patent
Jiangsu Chia Tai Fenghai Pharmaceutical
US Patent
Affinity DataIC50: 24.1nMAssay Description:Compounds of Formula I were screened for their ability to inhibit wildtype and V804M mutant RET kinase using CisBio's HTRF KinEASE -TK assay tech...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [V804M](Human)
Jiangsu Chia Tai Fenghai Pharmaceutical
US Patent
Jiangsu Chia Tai Fenghai Pharmaceutical
US Patent
Affinity DataIC50: 24.1nMAssay Description:RET: Compounds of Formula I were screened for their ability to inhibit wildtype and V804M mutant RET kinase using CisBio's HTRF KinEASE -TK assay...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affinity DataIC50: 29.3nMpH: 7.4Assay Description:Compounds of Formula I were screened for their ability to inhibit wildtype and V804M mutant RET kinase using CisBio's HTRF KinEASE -TK assay tech...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [V804M](Human)
Jiangsu Chia Tai Fenghai Pharmaceutical
US Patent
Jiangsu Chia Tai Fenghai Pharmaceutical
US Patent
TargetProto-oncogene tyrosine-protein kinase receptor Ret [G810R](Human)
Applied Pharmaceutical Science
US Patent
Applied Pharmaceutical Science
US Patent
Affinity DataIC50: 43.2nMAssay Description:1.3 Preparation of 1× Kinase Buffer4 volume of distilled water was added to 1 volume of enzyme buffer 5×; 5 mM MgCl2; 1 mM DTT.1.4 Screening Methoda)...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [G810R](Human)
Applied Pharmaceutical Science
US Patent
Applied Pharmaceutical Science
US Patent
Affinity DataIC50: 43.2nMAssay Description:a) 10 nL of compound dilution was transferred to each well of the test plate;b) the compound plate was centrifuged at 1000 g for 1 min;c) the test pl...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [G810R](Human)
Applied Pharmaceutical Science
US Patent
Applied Pharmaceutical Science
US Patent
Affinity DataIC50: 74nMAssay Description:The three drug-resistant mutant RET enzymes were each pre-incubated with different concentrations of test compounds (in the inhibition rate test of t...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [V804M](Human)
Jiangsu Chia Tai Fenghai Pharmaceutical
US Patent
Jiangsu Chia Tai Fenghai Pharmaceutical
US Patent
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affinity DataIC50: 95nMAssay Description:Inhibition of RET G810S mutant (unknown origin) by FRET-based ZLyte kinase assayMore data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Human)
University of Arkansas For Medical Sciences
Curated by ChEMBL
University of Arkansas For Medical Sciences
Curated by ChEMBL
Affinity DataIC50: 100nMAssay Description:Inhibition of recombinant VEGFR2 (unknown origin) incubated for 120 mins by Perkin Elmer electrophoretic mobility shift platform methodMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affinity DataIC50: 107nMAssay Description:Inhibition of RET G810C mutant (unknown origin) by FRET-based ZLyte kinase assayMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [G810C](Human)
Sichuan Kelun-Biotech Biopharmaceutical Co.
US Patent
Sichuan Kelun-Biotech Biopharmaceutical Co.
US Patent
Affinity DataIC50: 151nMAssay Description:The three drug-resistant mutant RET enzymes were each pre-incubated with different concentrations of test compounds (in the inhibition rate test of t...More data for this Ligand-Target Pair
TargetVascular endothelial growth factor receptor 2(Human)
University of Arkansas For Medical Sciences
Curated by ChEMBL
University of Arkansas For Medical Sciences
Curated by ChEMBL
Affinity DataIC50: 172nMAssay Description:The activity assay method for the above kinases was established by homogeneous time-resolved fluorescence (HTRF), and the inhibitory activity of the ...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affiliated Hengyang Hospital of Hunan Normal University & Hengyang Central Hospital
Curated by ChEMBL
Affinity DataIC50: 244nMAssay Description:Inhibition of RET G810R mutant (unknown origin) by FRET-based ZLyte kinase assayMore data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [G810R](Human)
Applied Pharmaceutical Science
US Patent
Applied Pharmaceutical Science
US Patent
Affinity DataIC50: 531nMAssay Description:The potency of a compound inhibiting G81 OR mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assays containe...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [G810R](Human)
Applied Pharmaceutical Science
US Patent
Applied Pharmaceutical Science
US Patent
Affinity DataIC50: 531nMAssay Description:Compounds of Formula I were screened for their ability to inhibit wildtype and V804M mutant RET kinase using CisBio's HTRF KinEASE -TK assay tech...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [G810R](Human)
Applied Pharmaceutical Science
US Patent
Applied Pharmaceutical Science
US Patent
Affinity DataIC50: 531nMAssay Description:RET G810R: The potency of a compound inhibiting G810R mutant RET kinase was determined using CisBio's HTRF Kinease-TK assay technology. The assay...More data for this Ligand-Target Pair
TargetProto-oncogene tyrosine-protein kinase receptor Ret [G810R](Human)
Applied Pharmaceutical Science
US Patent
Applied Pharmaceutical Science
US Patent
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Jiangsu Chia Tai Fenghai Pharmaceutical
US Patent
Jiangsu Chia Tai Fenghai Pharmaceutical
US Patent
Affinity DataIC50: 2.75E+3nMAssay Description:Inhibition of hERG Potassium Channel by Prepared Compounds The final concentrations of test compounds were all prepared on the day of experiment and ...More data for this Ligand-Target Pair