Compile Data Set for Download or QSAR
Report error Found 31 Enz. Inhib. hit(s) for PDB: 3OXZ
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)
TargetTyrosine-protein kinase ABL1(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of wild type human ABL Q252H mutant using [EAIYAAPFAKKK] as substrate in presence of gamma33P-ATP by radiometric HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase ABL1(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of wild type human ABL Y253F mutant using [EAIYAAPFAKKK] as substrate in presence of gamma33P-ATP by radiometric HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase ABL1(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of wild type human ABL M351T mutant using [EAIYAAPFAKKK] as substrate in presence of gamma33P-ATP by radiometric HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase ABL1(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 0.300nMAssay Description:Inhibition of wild type human ABL H396P mutant using [EAIYAAPFAKKK] as substrate in presence of gamma33P-ATP by radiometric HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase ABL1(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 0.310nMAssay 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
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase ABL1(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 0.330nMAssay Description:Inhibition of human recombinant wild type ABL1 expressed in insect cells after 30 mins by FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase ABL1(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 0.370nMAssay Description:Inhibition of recombinant wild type Abl (unknown origin) in presence of [33P]-ATP by radiometric hotspot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/19/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase ABL1(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 0.370nMAssay Description:Binding affinity to human ABL1 using EAIYAAPFAKKK as substrate by radiometric hotspot kinase assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/27/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase ABL1(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 0.370nMAssay Description:Inhibition of ABL (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase ABL1(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 0.370nMAssay Description:Inhibition of ABL autophosphorylationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/21/2010
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase ABL1(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 0.370nMAssay Description:Inhibition of wild type human ABL using [EAIYAAPFAKKK] as substrate in presence of gamma33P-ATP by radiometric HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase ABL1(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 0.370nMAssay Description:Inhibition of Abl (unknown origin) in presence of ATP by ADP Glo assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/20/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase ABL1(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 0.370nMAssay Description:Inhibition of recombinant human ABL using peptide substrate EAIYAAPFAKKK in presence of [33-P]ATP by kinase hotspot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/24/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
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)
TargetTyrosine-protein kinase ABL1(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 0.580nMAssay Description:Inhibition of breakpoint cluster region-Abelson tyrosine kinase T315I mutant (unknown origin) using [gamma-33P]ATP as substrate by radiometric kinase...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/31/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase ABL1 [229-512](Human)
Stony Brook University

LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataKd:  0.700nMAssay 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
PubMedPDB3D3D Structure (crystal)
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)
TargetTyrosine-protein kinase ABL1 [T315I](Human)
Nanjing Sanhome Pharmaceutical

US Patent
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 1nMT: 2°CAssay Description:Serially diluting the compound of the present invention from 1 uM initial concentration in three-fold fashion and formulating 10 concentrations (50.8...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/20/2016
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
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)
TargetTyrosine-protein kinase ABL1(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 1nMAssay Description:Inhibition of human ABL T315I mutant using EAIYAAPFAKKK substrate and [gamma-33P]-ATP incubated for 40 mins by scintillation counting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase ABL1(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 1.40nMAssay Description:Inhibition of Abl (unknown origin) incubated for 1 hr by ADP-Glo assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase ABL1(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 2nMAssay Description:Inhibition of recombinant Abl-T315I mutant (unknown origin) in presence of [33P]-ATP by kinase hotspot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/19/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase ABL1(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 2nMAssay Description:Inhibition of wild type human ABL T315I mutant using [EAIYAAPFAKKK] as substrate in presence of gamma33P-ATP by radiometric HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase ABL1(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 2.20nMAssay Description:Inhibition of recombinant human full-length His-tagged ABL1 cytoplasmic domain expressed in baculovirus expression system using Tyr 02 as substrate m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase ABL1(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 2.90nMAssay Description:Inhibition of human wild-type ABL (Ser229 to Gln513)-mediated phosphorylation of biotinylated poly-Glu-Tyr expressed in Escherichia coli BL21(DE3) pr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase ABL1(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 5.10nMAssay Description:Inhibition of recombinant human full-length His-tagged ABL1 T315I mutant cytoplasmic domain expressed in baculovirus infected insect cells using Tyr ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/23/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase ABL1(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 7.70nMAssay Description:Inhibition of recombinant ABL (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/16/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase ABL1(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 8.60nMAssay Description:Inhibition of wild type human ABL using [EAIYAAPFAKKK] peptide substrate by Hotspot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/5/2011
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase ABL1(Human)
Jinan University

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 8.60nMAssay Description:Inhibition of wild type human ABL after 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/21/2010
Entry Details Article
PubMedPDB3D3D Structure (crystal)