BDBM50507492 Loxo-195::Selitrectinib::US10966985, Compound 33-B

SMILES C[C@@H]1CCc2ncc(F)cc2[C@H]2CCCN2c2ccn3ncc(C(=O)N1)c3n2

InChI Key InChIKey=OEBIHOVSAMBXIB-UHFFFAOYSA-N

Data  62 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 97 hits for monomerid = 50507492   

TargetHigh affinity nerve growth factor receptor(Human)
National Health Research Institutes

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 0.0700nMAssay Description:Inhibition of wildtype human TRKA using poly (Glu,Tyr) 4:1 as substrate in presence of [gamma-33P]ATP by hotspot kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
TargetHigh affinity nerve growth factor receptor(Human)
National Health Research Institutes

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 0.470nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetProto-oncogene tyrosine-protein kinase ROS [D2033N](Human)
Array Biopharma

US Patent
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 0.5nMAssay Description:The potency of a compound inhibiting wild type and exemplary mutant ROS1 kinases was determined using CisBio's HTRF Kinease-TK assay technology. ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/9/2021
Entry Details
US Patent

TargetProto-oncogene tyrosine-protein kinase ROS [G2032R](Human)
Array Biopharma

US Patent
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 0.5nMAssay Description:The potency of a compound inhibiting wild type and exemplary mutant ROS1 kinases was determined using CisBio's HTRF Kinease-TK assay technology. ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/22/2021
Entry Details
US Patent

TargetNT-3 growth factor receptor(Human)
Yantai University

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 0.5nMAssay Description:Inhibition of TrKC (unknown origin) incubated for 120 mins in presence of 33P-ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/5/2023
Entry Details Article
PubMed
TargetHigh affinity nerve growth factor receptor(Human)
National Health Research Institutes

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 0.600nMAssay Description:Inhibition of His-tagged human recombinant wild type TRKAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/21/2024
Entry Details
PubMed
TargetHigh affinity nerve growth factor receptor(Human)
National Health Research Institutes

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 0.600nMAssay Description:Inhibition o wild type TRKA (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details

TargetHigh affinity nerve growth factor receptor(Human)
National Health Research Institutes

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 0.600nMAssay Description:Inhibition of N-terminal 6His-tagged wild type TRKA (486 to 786 residues) (unknown origin) expressed in Escherichia coli incubated for 60 mins by [ga...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details

TargetNT-3 growth factor receptor(Human)
Yantai University

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 0.700nMAssay Description:Inhibition of wild type TRKC (unknown origin) using TK peptide as substrate incubated for 30 mins in presence of ATP by HTRF analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details

TargetHigh affinity nerve growth factor receptor(Human)
National Health Research Institutes

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 0.900nMAssay Description:Inhibition of wild type TRKA (unknown origin) using TK peptide as substrate incubated for 30 mins in presence of ATP by HTRF analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details

TargetHigh affinity nerve growth factor receptor(Human)
National Health Research Institutes

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 0.900nMAssay Description:Inhibition of N-terminal GST-tagged human recombinant wild type TRKA (440 to end residues) expressed in baculovirus infected Sf9 insect cells incubat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/18/2024
Entry Details
PubMed
TargetHigh affinity nerve growth factor receptor(Human)
National Health Research Institutes

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 0.980nMAssay Description:Inhibition of TRKA G667C mutant (unknown origin) using poly-EAY peptide as substrate in presence of gamma-33ATP by LanthaScreen assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMed
TargetBDNF/NT-3 growth factors receptor(Human)
Yantai University

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 1nMAssay Description:Inhibition of wild-type TrKB (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/5/2023
Entry Details Article
PubMed
TargetNT-3 growth factor receptor(Human)
Yantai University

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 1nMAssay Description:Inhibition of wild-type TrKC (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/5/2023
Entry Details Article
PubMed
TargetBDNF/NT-3 growth factors receptor(Human)
Yantai University

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 1nMAssay Description:Inhibition of wild type TRKB (unknown origin) using TK peptide as substrate incubated for 30 mins in presence of ATP by HTRF analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details

TargetBDNF/NT-3 growth factors receptor(Human)
Yantai University

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 1nMAssay Description:Inhibition of wild type TRKB (unknown origin) using TK peptide as substrate incubated for 30 mins in presence of ATP by HTRF analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details

TargetHigh affinity nerve growth factor receptor(Human)
National Health Research Institutes

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 1nMAssay Description:Inhibition of wild type TRAK (unknown origin) incubated for 30 mins by caliper mobility shift assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/18/2024
Entry Details Article
PubMed
TargetNT-3 growth factor receptor(Human)
Yantai University

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 1nMAssay Description:Inhibition of wild type TRKC (unknown origin) using TK peptide as substrate incubated for 30 mins in presence of ATP by HTRF analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details

TargetHigh affinity nerve growth factor receptor(Human)
National Health Research Institutes

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 1nMAssay Description:Inhibition of wild-type TrKA (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/5/2023
Entry Details Article
PubMed
TargetNT-3 growth factor receptor(Human)
Yantai University

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 1nMAssay Description:Inhibition of TRKC (unknown origin) using TK as substrate incubated for 40 mins in presence of ATP by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details

TargetNT-3 growth factor receptor(Human)
Yantai University

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 1.10nMAssay Description:Inhibition of TRKC (unknown origin) using Ser/Thr 06 as peptide substrate incubated for 1 hr in presence of ATP by FRET based Z-LYTE assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/19/2024
Entry Details
PubMed
TargetProto-oncogene tyrosine-protein kinase ROS(Human)
Yantai University

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 1.20nMAssay Description:Inhibition of ROS1 (unknown origin) incubated for 120 mins in presence of 33P-ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/5/2023
Entry Details Article
PubMed
TargetNT-3 growth factor receptor(Human)
Yantai University

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 1.40nMAssay Description:Binding affinity to His-tagged recombinant wildtype human TRKC kinase domain incubated for 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details

TargetHigh affinity nerve growth factor receptor(Human)
National Health Research Institutes

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 1.60nMAssay Description:Inhibition of wildtype human extracellular domain deleted TRKA expressed in mouse NIH3T3 cells assessed as reduction in TRKA phosphorylation incubate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details

LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 1.60nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetBDNF/NT-3 growth factors receptor(Human)
Yantai University

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 1.90nMAssay Description:Binding affinity to wildtype TRKB (unknown origin) kinase domain incubated for 60 mins by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details

TargetHigh affinity nerve growth factor receptor(Human)
National Health Research Institutes

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 2nMAssay Description:Inhibition of TrKA G595R mutant (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/5/2023
Entry Details Article
PubMed
TargetBDNF/NT-3 growth factors receptor(Human)
Yantai University

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 2nMAssay Description:Inhibition of wild type TrkB (unknown origin) using poly(Glu: Tyr) as substrate preincubated for 15 mins followed by substrate addition and further i...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/6/2023
Entry Details Article
PubMed
TargetNT-3 growth factor receptor(Human)
Yantai University

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 2nMAssay Description:Inhibition of N-terminal His-tagged human recombinant TRKC (507 to end residues) expressed in baculovirus infected Sf9 insect cells incubated for 40 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/18/2024
Entry Details
PubMed
TargetHigh affinity nerve growth factor receptor(Human)
National Health Research Institutes

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 2nMAssay Description:Inhibition of TRKA (unknown origin) using TK as substrate incubated for 30 mins in presence of ATP by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details

TargetHigh affinity nerve growth factor receptor(Human)
National Health Research Institutes

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 2nMAssay Description:Inhibition of wild type TrkA (unknown origin) using poly(Glu: Tyr) as substrate preincubated for 15 mins followed by substrate addition and further i...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/6/2023
Entry Details Article
PubMed
TargetHigh affinity nerve growth factor receptor(Human)
National Health Research Institutes

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 2nMAssay Description:Inhibition of His-tagged human recombinant TRKA G595R mutantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/21/2024
Entry Details
PubMed
TargetHigh affinity nerve growth factor receptor(Human)
National Health Research Institutes

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 2nMAssay Description:Inhibition of N-terminal 6His-tagged TRKA G595R mutant (486 to 786 residues) (unknown origin) expressed in Escherichia coli incubated for 60 mins by ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details

TargetHigh affinity nerve growth factor receptor(Human)
National Health Research Institutes

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 2nMAssay Description:Inhibition of TRKA G595R mutant (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details

TargetHigh affinity nerve growth factor receptor(Human)
National Health Research Institutes

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 2nMAssay Description:Inhibition of TRKA G595R mutant (unknown origin) using poly-EAY peptide as substrate in presence of gamma-33ATP by LanthaScreen assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMed
TargetHigh affinity nerve growth factor receptor(Human)
National Health Research Institutes

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 2nMAssay Description:Inhibition of wild type N-terminal 6His-tagged TRKA G595R mutant (486 to 786 residues) (unknown origin) expressed in Escherichia coli measured after ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details

TargetHigh affinity nerve growth factor receptor(Human)
National Health Research Institutes

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 2.10nMAssay Description:Inhibition of TRKA G595R mutant (unknown origin) by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
TargetNT-3 growth factor receptor(Human)
Yantai University

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 2.30nMAssay Description:Inhibition of His-tagged human recombinant TRKC G623R mutantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/21/2024
Entry Details
PubMed
TargetNT-3 growth factor receptor(Human)
Yantai University

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 2.30nMAssay Description:Inhibition of wild type N-terminal 6His-tagged TRKC G623R mutant (506 to 829 residues) (unknown origin) expressed in Escherichia coli measured after ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details

TargetNT-3 growth factor receptor(Human)
Yantai University

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 2.40nMAssay Description:Inhibition of TRKC (unknown origin) using ser/thr 06 peptide as substrate incubated for 1 hr in presence of ATP by FRET based Z'-lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/22/2024
Entry Details
PubMed
TargetNT-3 growth factor receptor(Human)
Yantai University

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 2.40nMAssay Description:Inhibition of TRKC (unknown origin) using Ser/Thr 06 peptide as substrate incubated for 1 hr in presence of 50 uM ATP by FRET based Z'-Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
TargetNT-3 growth factor receptor(Human)
Yantai University

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 2.5nMAssay Description:Inhibition of N-terminal 6His-tagged wild type TRKC (506 to 829 residues) (unknown origin) expressed in Escherichia coli incubated for 60 mins by [ga...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details

TargetNT-3 growth factor receptor(Human)
Yantai University

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 2.5nMAssay Description:Inhibition of His-tagged human recombinant wild type TRKCMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/21/2024
Entry Details
PubMed
TargetNT-3 growth factor receptor [G623R](Homo sapiens (Human))TBA
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 2.5nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetProto-oncogene tyrosine-protein kinase ROS(Human)
Yantai University

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 2.70nMAssay Description:The potency of a compound inhibiting wild type and exemplary mutant ROS1 kinases was determined using CisBio's HTRF Kinease-TK assay technology. ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/9/2021
Entry Details
US Patent

TargetProto-oncogene tyrosine-protein kinase ROS(Human)
Yantai University

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 2.70nMAssay Description:The potency of a compound inhibiting wild type and exemplary mutant ROS1 kinases was determined using CisBio's HTRF Kinease-TK assay technology. ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/22/2021
Entry Details
US Patent

TargetNT-3 growth factor receptor(Human)
Yantai University

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 2.80nMAssay Description:Inhibition of TRKC (unknown origin) by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details

TargetHigh affinity nerve growth factor receptor(Human)
National Health Research Institutes

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 2.90nMAssay Description:Inhibition of TRKA (unknown origin) using ser/thr 06 peptide as substrate incubated for 1 hr in presence of ATP by FRET based Z'-lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/22/2024
Entry Details
PubMed
TargetHigh affinity nerve growth factor receptor(Human)
National Health Research Institutes

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 3nMAssay Description:Inhibition of N-terminal hexa his tagged TRKA (485 to 795 residues) (unknown origin) expressed in baculovirus expression system Sf9 cells using Ser/T...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/19/2024
Entry Details
PubMed
TargetNT-3 growth factor receptor(Human)
Yantai University

Curated by ChEMBL
LigandPNGBDBM50507492(Loxo-195 | Selitrectinib | US10966985, Compound 33...)
Affinity DataIC50: 3nMAssay Description:Inhibition of wild type TrkC (unknown origin) using poly(Glu: Tyr) as substrate preincubated for 15 mins followed by substrate addition and further i...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/6/2023
Entry Details Article
PubMed
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