Compile Data Set for Download or QSAR
Report error Found 962 Enz. Inhib. hit(s) with Target = 'Breakpoint cluster region protein'
LigandPNGBDBM50172492(CHEMBL3808884)
Affinity DataEC50:  0.0400nMAssay Description:Inhibition of human wild type BCR-ABL expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/5/2017
Entry Details Article
PubMed
LigandPNGBDBM13216(N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyeth...)
Affinity DataEC50:  0.0400nMAssay Description:Inhibition of human wild type BCR-ABL expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/5/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataEC50:  0.0500nMAssay Description:Inhibition of human wild type BCR-ABL expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/5/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataEC50:  0.300nMAssay Description:Inhibition of human BCR-ABL T315I mutant expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/5/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
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
LigandPNGBDBM50399374(CHEMBL2178270)
Affinity DataIC50: 0.330nMAssay Description:Inhibition of wild type Bcr-Abl using Tyr2 peptide as substrate after 2 hrs by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandPNGBDBM50399367(CHEMBL2178277)
Affinity DataIC50: 0.360nMAssay Description:Inhibition of wild type Bcr-Abl using Tyr2 peptide as substrate after 2 hrs by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandPNGBDBM50399373(CHEMBL2178271)
Affinity DataIC50: 0.410nMAssay Description:Inhibition of wild type Bcr-Abl using Tyr2 peptide as substrate after 2 hrs by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandPNGBDBM50399368(CHEMBL2178276)
Affinity DataIC50: 0.420nMAssay Description:Inhibition of wild type Bcr-Abl using Tyr2 peptide as substrate after 2 hrs by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandPNGBDBM50459091(ABL-001 | ABL001 | ABL001-NX | Asciminib | NVP-ABL...)
Affinity DataKd:  0.450nMAssay Description:Binding affinity to BCR-ABL1 (unknown origin) assessed as dissociation constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/21/2023
Entry Details
PubMed
LigandPNGBDBM50399379(CHEMBL2177649)
Affinity DataIC50: 0.450nMAssay Description:Inhibition of wild type Bcr-Abl using Tyr2 peptide as substrate after 2 hrs by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandPNGBDBM50399376(CHEMBL2178268)
Affinity DataIC50: 0.450nMAssay Description:Inhibition of wild type Bcr-Abl using Tyr2 peptide as substrate after 2 hrs by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandPNGBDBM50591914(CHEMBL5208315)
Affinity DataIC50: 0.490nMAssay Description:Inhibition of wild type Bcr-Abl (unknown origin) incubated for 1 hr in presence of ATP by ADP-Glo kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2023
Entry Details
PubMed
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 0.5nMAssay Description:Inhibition of BCR-ABL (unknown origin) by kinase hotspot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/24/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50399380(CHEMBL2177648)
Affinity DataIC50: 0.520nMAssay Description:Inhibition of wild type Bcr-Abl using Tyr2 peptide as substrate after 2 hrs by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandPNGBDBM50399396(CHEMBL2177632)
Affinity DataIC50: 0.520nMAssay Description:Inhibition of wild type Bcr-Abl using Tyr2 peptide as substrate after 2 hrs by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandPNGBDBM50399382(CHEMBL2177646)
Affinity DataIC50: 0.520nMAssay Description:Inhibition of wild type Bcr-Abl using Tyr2 peptide as substrate after 2 hrs by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandPNGBDBM50433237(CHEMBL2375971)
Affinity DataIC50: 0.520nMAssay 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
LigandPNGBDBM50399375(CHEMBL2178269)
Affinity DataIC50: 0.520nMAssay Description:Inhibition of wild type Bcr-Abl using Tyr2 peptide as substrate after 2 hrs by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandPNGBDBM50399394(CHEMBL2177634)
Affinity DataIC50: 0.540nMAssay Description:Inhibition of wild type Bcr-Abl using Tyr2 peptide as substrate after 2 hrs by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandPNGBDBM50591905(CHEMBL5206449)
Affinity DataIC50: 0.600nMAssay Description:Inhibition of wild type Bcr-Abl (unknown origin) incubated for 1 hr in presence of ATP by ADP-Glo kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2023
Entry Details
PubMed
LigandPNGBDBM50399383(CHEMBL2177645)
Affinity DataIC50: 0.600nMAssay Description:Inhibition of wild type Bcr-Abl using Tyr2 peptide as substrate after 2 hrs by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandPNGBDBM50591878(CHEMBL5182032)
Affinity DataIC50: 0.650nMAssay Description:Inhibition of wild type Bcr-Abl (unknown origin) incubated for 1 hr in presence of ATP by ADP-Glo kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2023
Entry Details
PubMed
LigandPNGBDBM50399386(CHEMBL2177642)
Affinity DataIC50: 0.690nMAssay Description:Inhibition of wild type Bcr-Abl using Tyr2 peptide as substrate after 2 hrs by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandPNGBDBM50399366(CHEMBL2178278)
Affinity DataIC50: 0.700nMAssay Description:Inhibition of wild type Bcr-Abl using Tyr2 peptide as substrate after 2 hrs by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandPNGBDBM50399381(CHEMBL2177647)
Affinity DataIC50: 0.720nMAssay Description:Inhibition of wild type Bcr-Abl using Tyr2 peptide as substrate after 2 hrs by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandPNGBDBM50399395(CHEMBL2177633)
Affinity DataIC50: 0.780nMAssay Description:Inhibition of wild type Bcr-Abl using Tyr2 peptide as substrate after 2 hrs by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandPNGBDBM13216(N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyeth...)
Affinity DataIC50: 0.800nMAssay 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
PubMed
LigandPNGBDBM13216(N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyeth...)
Affinity DataIC50: 0.800nMAssay Description:Inhibition of wild type Bcr-AblMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/18/2010
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50591892(CHEMBL5200499)
Affinity DataIC50: 0.830nMAssay Description:Inhibition of wild type Bcr-Abl (unknown origin) incubated for 1 hr in presence of ATP by ADP-Glo kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2023
Entry Details
PubMed
LigandPNGBDBM50590370(Vodobatinib | K-0706 | K0706 | Sco-088 | VODOBATIN...)
Affinity DataIC50: 0.900nMAssay Description:Inhibition of wild type BCR-ABL phosphorylation in mouse BaF3 cells incubated for 4 hrs by immunoblotting analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/19/2023
Entry Details
PubMed
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 0.900nMAssay Description:Inhibition of Bcr-Abl T315I mutant (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
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50591875(CHEMBL5179613)
Affinity DataIC50: 0.940nMAssay Description:Inhibition of wild type Bcr-Abl (unknown origin) incubated for 1 hr in presence of ATP by ADP-Glo kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/20/2023
Entry Details
PubMed
LigandPNGBDBM50399365(CHEMBL2178279)
Affinity DataIC50: 0.980nMAssay Description:Inhibition of wild type Bcr-Abl using Tyr2 peptide as substrate after 2 hrs by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
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
LigandPNGBDBM13216(N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyeth...)
Affinity DataIC50: 1nMAssay Description:Inhibition of Bcr-Abl kinaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM50462183(CHEMBL3736320)
Affinity DataEC50:  1nMAssay Description:Inhibition of wild-type Bcr-Abl autophosphorylation (unknown origin) expressed in mouse BA/F3 cells for 3 hrs by Western blot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/4/2020
Entry Details Article
PubMed
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 1nMAssay 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
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM13216(N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyeth...)
Affinity DataIC50: 1nMAssay Description:Inhibition of BCR-ABL phosphorylation in human K562 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/19/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetBreakpoint cluster region protein [1-693](Human)
St. Chuan University

US Patent
LigandPNGBDBM50086441(CHEMBL3426225 | US10266537, Compound 3)
Affinity DataIC50: 1nMAssay Description:The aim of this experiment is to detect the inhibitory activity of the compounds of the present invention against in vitro protein kinases using isot...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2020
Entry Details
US Patent

LigandPNGBDBM50399369(CHEMBL2178275)
Affinity DataIC50: 1.01nMAssay Description:Inhibition of wild type Bcr-Abl using Tyr2 peptide as substrate after 2 hrs by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandPNGBDBM50399392(CHEMBL2177636)
Affinity DataIC50: 1.01nMAssay Description:Inhibition of wild type Bcr-Abl using Tyr2 peptide as substrate after 2 hrs by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandPNGBDBM50399371(CHEMBL2178273)
Affinity DataIC50: 1.03nMAssay Description:Inhibition of wild type Bcr-Abl using Tyr2 peptide as substrate after 2 hrs by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandPNGBDBM13530(cid_5291 | STI571 | N-(4-methyl-3-{[4-(pyridin-3-y...)
Affinity DataIC50: 1.10nMAssay Description:Inhibition of wild type Bcr-AblMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/18/2010
Entry Details Article
PubMed
LigandPNGBDBM50399393(CHEMBL2177635)
Affinity DataIC50: 1.18nMAssay Description:Inhibition of wild type Bcr-Abl using Tyr2 peptide as substrate after 2 hrs by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandPNGBDBM50590368(Radotinib | IY5511 | RADOTINIB)
Affinity DataIC50: 1.20nMAssay 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
LigandPNGBDBM50529313(Flumatinib | HH-GV678 | Hhgv-678)
Affinity DataIC50: 1.20nMAssay Description:Inhibition of BCR-ABL phosphorylation in human K562 cells incubated for 3 hrs by Western blot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/19/2023
Entry Details
PubMed
LigandPNGBDBM50323777(N-(4-Methyl-3-(1-methyl-7-(6-methylpyridin-3-ylami...)
Affinity DataIC50: 1.25nMAssay Description:Inhibition of wild type Bcr-AblMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandPNGBDBM50323777(N-(4-Methyl-3-(1-methyl-7-(6-methylpyridin-3-ylami...)
Affinity DataIC50: 1.25nMAssay Description:Inhibition of wild type Bcr-Abl using Tyr2 peptide as substrate after 2 hrs by FRET-based Z'-Lyte assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandPNGBDBM4552(CHEMBL288441 | SKI-606 | 4-[(2,4-Dichloro-5-methox...)
Affinity DataIC50: 1.40nMAssay Description:Inhibition of BCR-ABL (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/19/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
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