BDBM136597 US10005783, 14::US10047097, 14::US10774085, Example 14::US11098046, Compound LOXO-101::US11267818, Example 14::US11453672, Example L-7::US8865698, 14::US9676783, 14

SMILES O[C@H]1CCN(C1)C(=O)Nc1cnn2ccc(nc12)N1CCC[C@@H]1c1cc(F)ccc1F

InChI Key InChIKey=NYNZQNWKBKUAII-KBXCAEBGSA-N

Data  78 IC50

  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 78 hits for monomerid = 136597   

TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  9.70nMpH: 7.5Assay Description:An enzyme-linked immunosorbant assay (ELISA) was used to assess TrkA kinase activity in the presence of inhibitors. Immulon 4HBX 384-well microtiter ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  9.70nMpH: 7.5Assay Description:An enzyme-linked immunosorbant assay (ELISA) was used to assess TrkA kinase activity in the presence of inhibitors. Immulon 4HBX 384-well microtiter ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHigh affinity nerve growth factor receptor [441-796](Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  9.70nMpH: 7.5Assay Description:Immulon 4HBX 384-well microtiter plates (Thermo part #8755) were coated with a 0.025 mg/mL solution of poly (Glu, Ala, Tyr; 6:3:1; Sigma P3899). Vari...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBDNF/NT-3 growth factors receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  24nMAssay Description:Inhibition of TrkB (unknown origin) by cell based assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNT-3 growth factor receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  24nMAssay Description:Inhibition of TrkC (unknown origin) by cell based assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  9.70nMAssay Description:Inhibition of TrkA (unknown origin) by cell based assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  9.70nMAssay Description:Trk enzymatic selectivity was assessed using Omnia Kinase Assay reagents from Invitrogen Corp. Enzyme (either TrkA or TrkB from Invitrogen Corp.) and...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  2nMAssay Description:Inhibition of TRKA (unknown origin) assessed as reduction in incorporation of [33P]PO4 from [gamma-33P]-ATP using poly-EAY peptide as substrate by Fl...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  3.30nMAssay Description:Inhibition of recombinant human His-tagged TrkA catalytic domain (441 to 796 residues) expressed in baculovirus expression system using tyr 01 as sub...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNT-3 growth factor receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  3.5nMAssay Description:Inhibition of recombinant human His-tagged TrkC cytoplasmic domain (510 to 825 residues) expressed in baculovirus using tyr 01 as substrate incubated...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBDNF/NT-3 growth factors receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  5.20nMAssay Description:Inhibition of recombinant human His-tagged TrkB catalytic domain (526 to 838 residues) expressed in baculovirus expression system using tyr 01 as sub...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase ABL1(Homo sapiens (Human))
Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50: >1.00E+3nMAssay Description:Inhibition of recombinant full length human His-tagged ABL1 expressed in baculovirus infected insect cells using tyr 02 as substrate incubated for 2 ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  2nMAssay Description:Inhibition of TRKA (unknown origin) by FISH assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  45nMAssay 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 DepthDetails ArticlePubMed
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  69nMAssay 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 DepthDetails ArticlePubMed
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  9.70nMAssay Description:An enzyme-linked immunosorbant assay (ELISA) was used to assess TrkA kinase activity in the presence of inhibitors. Immulon 4HBX 384-well microtiter ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  2.90nMAssay Description:Inhibition of TrkA (unknown origin) using Tyr1 peptide as substrate in presence of ATP measured after 2 hrs by FRET-based Z-Lyte kinase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBDNF/NT-3 growth factors receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  2.30nMAssay Description:Inhibition of TrkB (unknown origin) using Tyr1 peptide as substrate in presence of ATP measured after 2 hrs by FRET-based Z-Lyte kinase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNT-3 growth factor receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  1.70nMAssay Description:Inhibition of TrkC (unknown origin) using Tyr1 peptide as substrate in presence of ATP measured after 2 hrs by FRET-based Z-Lyte kinase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  5.90nMAssay Description:The HotSpot assay platform was used to measure kinase/inhibitor interactions as described in Anastassiadis et al., Nat Biotechnol. 29:1039-45, 2011. ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetNT-3 growth factor receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  2.10nMAssay Description:Inhibition of Trk-C (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBDNF/NT-3 growth factors receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  2.10nMAssay Description:Inhibition of Trk-B (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  1.20nMAssay Description:Inhibition of Trk-A (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  9.70nMAssay Description:An enzyme-linked immunosorbant assay (ELISA) was used to assess TrkA kinase activity in the presence of inhibitors. Immulon 4HBX 384-well microtiter ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  0.900nMAssay Description:Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of the compound prepared by pre-diluting, and allowed...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBDNF/NT-3 growth factors receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  0.540nMAssay Description:Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of the compound prepared by pre-diluting, and allowed...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetNT-3 growth factor receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  0.440nMAssay Description:Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of the compound prepared by pre-diluting, and allowed...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  0.820nMAssay Description:Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of the compound prepared by pre-diluting, and allowed...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBDNF/NT-3 growth factors receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  0.460nMAssay Description:Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of the compound prepared by pre-diluting, and allowed...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetNT-3 growth factor receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  0.410nMAssay Description:Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of the compound prepared by pre-diluting, and allowed...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  0.960nMAssay Description:Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of the compound prepared by pre-diluting, and allowed...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBDNF/NT-3 growth factors receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  0.460nMAssay Description:Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of the compound prepared by pre-diluting, and allowed...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetNT-3 growth factor receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  0.450nMAssay Description:Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of the compound prepared by pre-diluting, and allowed...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  1.13nMAssay Description:Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of the compound prepared by pre-diluting, and allowed...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBDNF/NT-3 growth factors receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  0.400nMAssay Description:Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of the compound prepared by pre-diluting, and allowed...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetNT-3 growth factor receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  0.320nMAssay Description:Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of the compound prepared by pre-diluting, and allowed...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  0.730nMAssay Description:Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of the compound prepared by pre-diluting, and allowed...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBDNF/NT-3 growth factors receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  0.330nMAssay Description:Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of the compound prepared by pre-diluting, and allowed...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetNT-3 growth factor receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  0.290nMAssay Description:Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of the compound prepared by pre-diluting, and allowed...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  0.860nMAssay Description:Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of the compound prepared by pre-diluting, and allowed...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBDNF/NT-3 growth factors receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  0.630nMAssay Description:Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of the compound prepared by pre-diluting, and allowed...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetNT-3 growth factor receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  0.290nMAssay Description:Kinase assay: After the buffer was prepared, the enzyme was mixed with different concentrations of the compound prepared by pre-diluting, and allowed...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  1.20nMAssay Description:Inhibition of wildtype TRKA (unknown origin) preincubated for 30 mins followed by biotinylated TK-peptide substrate addition and measured after 40 mi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  109nMAssay Description:Inhibition of TRKA GS95R mutant (unknown origin) preincubated for 30 mins followed by biotinylated TK-peptide substrate addition and measured after 4...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  32nMAssay Description:Inhibition of TRKA G667C mutant (unknown origin) preincubated for 30 mins followed by biotinylated TK-peptide substrate addition and measured after 4...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNT-3 growth factor receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  5nMAssay Description:Inhibition of wild type TRKC (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  5nMAssay Description:Inhibition of wild type TRKA (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBDNF/NT-3 growth factors receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  5nMAssay Description:Inhibition of wild type TRKB (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  237nMAssay Description:Inhibition of TRKA G595R mutant (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Array Biopharma

US Patent
LigandPNGBDBM136597(US10005783, 14 | US10047097, 14 | US10774085, Exam...)
Affinity DataIC50:  5nMAssay Description:Inhibition of TrkA (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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