BDBM50237710 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide::AMN 107::AMN107::CHEMBL255863::NILOTINIB::US11649218, Example Nilotinib

SMILES Cc1cn(cn1)-c1cc(NC(=O)c2ccc(C)c(Nc3nccc(n3)-c3cccnc3)c2)cc(c1)C(F)(F)F

InChI Key InChIKey=HHZIURLSWUIHRB-UHFFFAOYSA-N

Data  38 KI  69 IC50  457 Kd  1 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 614 hits for monomerid = 50237710   

TargetBreakpoint cluster region protein/Tyrosine-protein kinase ABL1(Human)
Xi'An Jiaotong University

Curated by ChEMBL
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 0.330nMAssay Description:Inhibition of Bcr-Abl kinase (unknown origin) after 30 mins by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/12/2014
Entry Details Article
PubMed
TargetDiscoidin domain-containing receptor 2(Human)
Massachusetts General Hospital and Harvard Medical School

LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 0.5nMAssay Description:Tet inducible human DDR1 over-expressing U2OS was pre-treated by media containing each of the compound for 1 hour and treated by changing the media t...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2014
Entry Details Article
PubMed
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 0.870nMAssay Description:Inhibition of human N-terminal his tagged unphosphorylated native ABL1 (229 to 499 residues) expressed in Sf9 cells using ABLtide as substrate preinc...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetBreakpoint cluster region protein/Tyrosine-protein kinase ABL1(Human)
Xi'An Jiaotong University

Curated by ChEMBL
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 1nMAssay Description:Inhibition of BCR-ABL (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/19/2023
Entry Details
PubMed
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
In Depth
Date in BDB:
6/10/2012
Entry Details Article
PubMed
TargetEpithelial discoidin domain-containing receptor 1(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataKd:  1.10nMAssay Description:Binding constant for DDR1 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 1.10nMAssay Description:Inhibition of human ABL1 H396P mutant (229 to 499 residues) using ABLtide as substrate preincubated for 2 hrs followed by ATP addition and measured e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 1.20nMAssay Description:Inhibition of recombinant human N-terminal His-tagged Abl (2 to 1130 residues) expressed in baculovirus expression system using FAM-labelled P2 pepti...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/14/2021
Entry Details Article
PubMed
TargetMast/stem cell growth factor receptor Kit(Human)
Genomics Institute of The Novartis Research Foundation

Curated by PDSP Ki Database
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
In Depth
Date in BDB:
6/10/2012
Entry Details Article
PubMed
TargetPlatelet-derived growth factor receptor alpha(Human)
Genomics Institute of The Novartis Research Foundation

Curated by PDSP Ki Database
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
In Depth
Date in BDB:
6/10/2012
Entry Details Article
PubMed
TargetDiscoidin domain-containing receptor 2(Human)
Massachusetts General Hospital and Harvard Medical School

LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 2nMAssay Description:Inhibition of wild type DDR2 (unknown origin) preincubated for 30 mins before substrate addition by FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2015
Entry Details Article
PubMed
TargetPlatelet-derived growth factor receptor beta(Human)
Genomics Institute of The Novartis Research Foundation

Curated by PDSP Ki Database
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
In Depth
Date in BDB:
6/10/2012
Entry Details Article
PubMed
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 2.20nMAssay Description:Inhibition of human N-terminal his tagged phosphorylated native ABL1 (229 to 499 residues) expressed in Sf9 cells using ABLtide as substrate preincub...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataKd:  3.60nMAssay Description:Binding affinity to human ABL1More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetEpithelial discoidin domain-containing receptor 1(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 3.70nMAssay Description:Inhibition of autophosphorylation of DDR1 expressed in HEK293 cells by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/12/2011
Entry Details Article
PubMed
TargetEphrin type-B receptor 2(Human)
Genomics Institute of The Novartis Research Foundation

Curated by PDSP Ki Database
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
In Depth
Date in BDB:
6/10/2012
Entry Details Article
PubMed
TargetCarbonic anhydrase 2(Human)
University of Tampere and Tampere University Hospital

Curated by ChEMBL
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataKi:  4.10nMAssay Description:Inhibition of human carbonic anhydrase 2 by stopped flow CO2 hydration assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/26/2010
Entry Details Article
PubMed
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataKd:  4.90nMAssay Description:Binding affinity to ABL1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMed
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataKd:  4.90nMAssay Description:Binding constant for ABL1(H396P)-non phosphorylated kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 5.15nMAssay Description:Compounds were tested against the Abl1 target kinase and showed potencies between 0.30 and 0.64 nanomolar, compared to nilotinib which showed a poten...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetDiscoidin domain-containing receptor 2(Human)
Massachusetts General Hospital and Harvard Medical School

LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 5.20nMAssay Description:Inhibition of autophosphorylation of DDR2 expressed in HEK293 cells by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/12/2011
Entry Details Article
PubMed
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 5.60nMAssay Description:Inhibition of human ABL1 assessed as residual activity using EAIYAAPFAKKK as substrate by [gamma-33P]-ATP assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/11/2021
Entry Details Article
PubMed
TargetDiscoidin domain-containing receptor 2(Human)
Massachusetts General Hospital and Harvard Medical School

LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataKd:  6nMAssay Description:Binding affinity to wild type DDR2 (unknown origin) by FLiK assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/9/2015
Entry Details Article
PubMed
TargetDiscoidin domain-containing receptor 2(Human)
Massachusetts General Hospital and Harvard Medical School

LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataKd:  6.20nMAssay Description:Binding affinity to human DDR2More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 6.67nMAssay Description:Compounds were tested against the Abl1 target kinase and showed potencies between 0.30 and 0.64 nanomolar, compared to nilotinib which showed a poten...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 7nMAssay Description:Inhibition of GST tagged WT Abl (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]ATP additio...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 9nMAssay Description:Inhibition of GST tagged Abl M351T mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]A...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 9nMAssay Description:Inhibition of GST tagged Abl H396P mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate pre...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 10nMAssay Description:Inhibition of WT BCR-ABL (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of tyrosine phosphorylation incubated for 3 hrs by imm...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataKd:  10nMAssay Description:Binding constant for ABL1-non phosphorylated kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataKd:  10nMAssay Description:Binding constant for ABL1(Q252H)-non phosphorylated kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
TargetTyrosine-protein kinase ABL1 [229-512](Human)
Stony Brook University

LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataKd:  11nMAssay Description:Inhibitor selectivity profiles were obtained through Luceome Biotechnologies (Tuscon, AZ). Each inhibitor was screened at 0.5 μM against a panel...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/5/2016
Entry Details Article
PubMed
TargetMitogen-activated protein kinase kinase kinase 20(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataKd:  11nMAssay Description:Binding constant for ZAK kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 12nMAssay Description:Inhibition of GST tagged Abl M351T mutant (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate pre...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataKd:  12nMAssay Description:Binding constant for ABL1(F317L)-non phosphorylated kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataKd:  13nMAssay Description:Binding constant for ABL1-phosphorylated kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
TargetBreakpoint cluster region protein/Tyrosine-protein kinase ABL1(Human)
Xi'An Jiaotong University

Curated by ChEMBL
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 13nMAssay Description:Inhibition of wild type BCR/Abl (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/25/2021
Entry Details Article
PubMed
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataKd:  13nMAssay Description:Binding constant for ABL1(Y253F)-phosphorylated kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 13nMAssay Description:Inhibition of WT BCR-ABL (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by methane-thiosul...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 13nMAssay Description:Inhibition of GST tagged Abl M244V mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]A...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetBreakpoint cluster region protein/Tyrosine-protein kinase ABL1(Human)
Xi'An Jiaotong University

Curated by ChEMBL
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 14nMAssay Description:Inhibition of wild type Bcr-Abl (unknown origin) using Tyr2 peptide substrate after 2 hrs by FRET-based Z'-lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/17/2016
Entry Details Article
PubMed
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataKd:  14nMAssay Description:Binding constant for ABL1(F317L)-phosphorylated kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 15nMAssay Description:Inhibition of GST tagged WT Abl (unknown origin) assessed as inhibition of phosphorylation using biotin-EAIYAAPFAKKK-amide as substrate preincubated ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataKd:  15nMAssay Description:Binding constant for ABL1(M351T)-phosphorylated kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
TargetMast/stem cell growth factor receptor Kit(Human)
Genomics Institute of The Novartis Research Foundation

Curated by PDSP Ki Database
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 15nMAssay Description:Inhibition of human c-Kit using poly[Glu:Tyr] (4:1) peptide substrateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetEphrin type-B receptor 1(Human)
Genomics Institute of The Novartis Research Foundation

Curated by PDSP Ki Database
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataKi:  15nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/10/2012
Entry Details Article
PubMed
TargetTyrosine-protein kinase ABL1 [229-512](Human)
Stony Brook University

LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataKd:  15nMAssay Description:Inhibitor selectivity profiles were obtained through Luceome Biotechnologies (Tuscon, AZ). Each inhibitor was screened at 0.5 μM against phospho...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/5/2016
Entry Details Article
PubMed
TargetPlatelet-derived growth factor receptor beta(Human)
Genomics Institute of The Novartis Research Foundation

Curated by PDSP Ki Database
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataKd:  16nMAssay Description:Binding affinity to human PDGFRbeataMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataIC50: 17nMAssay Description:Inhibition of GST tagged Abl F311L mutant (unknown origin) assessed as inhibition of phosphorylation preincubated for 5 mins followed by [gamma-32P]A...More data for this Ligand-Target Pair
In Depth
Date in BDB:
TBA
Entry Details
TargetMast/stem cell growth factor receptor Kit(Human)
Genomics Institute of The Novartis Research Foundation

Curated by PDSP Ki Database
LigandPNGBDBM50237710(AMN 107 | AMN107 | 4-methyl-N-[3-(4-methyl-1H-imid...)
Affinity DataKd:  17nMAssay Description:Binding affinity to human c-KitMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
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