Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 918 hits for monomerid = 31093,47238,50097413,50097414,50097418,50277545,31093,47238,50097413,50097414,50097418,50277545   

TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM50277545(Alisertib | MLN8237 | CHEMBL483158 | 4-(9-chloro-7...)
Affinity DataIC50: 0.0400nMAssay Description:Inhibition of His-tagged human Aurora A kinase (122 to 40 residues) expressed in Escherichia coli BL21 (DE3) Rosetta cells using biotinylated STK2 su...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/18/2018
Entry Details Article
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM50277545(Alisertib | MLN8237 | CHEMBL483158 | 4-(9-chloro-7...)
Affinity DataKi:  0.136nM ΔG°:  -13.7kcal/mole IC50: 34.2nMT: 2°CAssay Description:Threefold dilution series of inhibitors in assay buffer were prepared in wells of a microtiter plate (final concentration stating from 2uM), and TAMR...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/16/2014
Entry Details Article
PubMed
TargetAurora kinase A(Mouse)
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50277545(Alisertib | MLN8237 | CHEMBL483158 | 4-(9-chloro-7...)
Affinity DataKi:  0.300nMAssay Description:Competitive inhibition of recombinant mouse aurora kinase A expressed in insect Sf9 cells in presence of ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/22/2016
Entry Details Article
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM47238(US9012475, MLN8237)
Affinity DataIC50: 0.600nMpH: 7.4Assay Description:The method for measuring the in-vitro inhibitory activity of a test compound against Aurora B kinase activity was substantially the same as in the ca...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/2/2015
Entry Details
Go to US Patent

TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM50277545(Alisertib | MLN8237 | CHEMBL483158 | 4-(9-chloro-7...)
Affinity DataIC50: 0.600nMpH: 7.4 T: 2°CAssay Description:For in vitro method for measuring the inhibitory activity of the aforementioned compounds on the aurora A kinase activity was carried out referring t...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/5/2017
Entry Details
Go to US Patent

TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM50277545(Alisertib | MLN8237 | CHEMBL483158 | 4-(9-chloro-7...)
Affinity DataIC50: 0.600nMpH: 7.4 T: 2°CAssay Description:For in vitro method for measuring the inhibitory activity of the aforementioned compounds on the aurora A kinase activity was carried out referring t...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/18/2019
Entry Details
Go to US Patent

TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM50277545(Alisertib | MLN8237 | CHEMBL483158 | 4-(9-chloro-7...)
Affinity DataIC50: 0.690nMT: 2°CAssay Description:Threefold dilution series of inhibitors in assay buffer were prepared in wells of a microtiter plate (final concentration stating from 2uM). Subseque...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/16/2014
Entry Details Article
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM50277545(Alisertib | MLN8237 | CHEMBL483158 | 4-(9-chloro-7...)
Affinity DataIC50: 1nMAssay Description:Inhibition of aurora A (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM50277545(Alisertib | MLN8237 | CHEMBL483158 | 4-(9-chloro-7...)
Affinity DataIC50: 1nMAssay Description:Inhibition of aurora A kinaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/22/2012
Entry Details Article
PubMed
TargetAurora kinase A(Mouse)
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50277545(Alisertib | MLN8237 | CHEMBL483158 | 4-(9-chloro-7...)
Affinity DataIC50: 1nMAssay Description:Inhibition of recombinant mouse aurora kinase A expressed in insect Sf9 cells using biotin-GLRRASLG as substrate in presence of [gamma-33P]ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/22/2016
Entry Details Article
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM50277545(Alisertib | MLN8237 | CHEMBL483158 | 4-(9-chloro-7...)
Affinity DataIC50: 1nMAssay Description:Inhibition of aurora A (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/2/2016
Entry Details Article
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataIC50: 1nMpH: 7.5 T: 2°CAssay Description:Aurora kinase was assayed in ELISA format using a GST fusion of the N-terminus of Histone H3 as substrate. Plates were coated with substrate, and the...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/28/2009
Entry Details Article
PubMed
TargetAurora kinase B/Inner centromere protein(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM50277545(Alisertib | MLN8237 | CHEMBL483158 | 4-(9-chloro-7...)
Affinity DataIC50: 1.10nMAssay Description:Inhibition of Aurora-B/INCENP (unknown origin) using biotinylated STK2 substrate incubated for 30 mins by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/18/2018
Entry Details Article
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM50277545(Alisertib | MLN8237 | CHEMBL483158 | 4-(9-chloro-7...)
Affinity DataIC50: 1.20nMAssay Description:Inhibition of Aurora A (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM50277545(Alisertib | MLN8237 | CHEMBL483158 | 4-(9-chloro-7...)
Affinity DataIC50: 1.20nMAssay Description:Inhibition of Aurora A kinase (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM50277545(Alisertib | MLN8237 | CHEMBL483158 | 4-(9-chloro-7...)
Affinity DataIC50: 1.20nMAssay Description:Inhibition of AURA (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM50277545(Alisertib | MLN8237 | CHEMBL483158 | 4-(9-chloro-7...)
Affinity DataIC50: 1.20nMAssay Description:Inhibition of recombinant Aurora A (unknown origin) by radioactive flashplate assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/13/2021
Entry Details Article
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM50277545(Alisertib | MLN8237 | CHEMBL483158 | 4-(9-chloro-7...)
Affinity DataIC50: 1.20nMAssay Description:Inhibition of Aurora A (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/21/2022
Entry Details Article
PubMed
TargetAurora kinase B(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM50277545(Alisertib | MLN8237 | CHEMBL483158 | 4-(9-chloro-7...)
Affinity DataIC50: 1.5nMAssay Description:Inhibition of Aurora B kinase in human HeLa Kyoto cells assessed as effect on distribution of phspho-histone H3 ser10 level incubated for 20 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/18/2018
Entry Details Article
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataIC50: 1.5nMAssay Description:Inhibition of aurora A kinaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2013
Entry Details Article
PubMed
LigandPNGBDBM50277545(Alisertib | MLN8237 | CHEMBL483158 | 4-(9-chloro-7...)
Affinity DataKi:  1.86nM ΔG°:  -12.1kcal/mole IC50: 1.78E+3nMT: 2°CAssay Description:Threefold dilution series of inhibitors in assay buffer were prepared in wells of a microtiter plate (final concentration stating from 2uM), and TAMR...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/16/2014
Entry Details Article
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataIC50: 3nMAssay Description:In vitro kinase assay of Aurora A, B, and C using Z-LYTE technology (Invitrogen) and ATP at Km apparent for each kinase.More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/4/2012
Entry Details Article
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM50277545(Alisertib | MLN8237 | CHEMBL483158 | 4-(9-chloro-7...)
Affinity DataIC50: 3.5nMT: 2°CAssay Description:Inhibition of Aurora A was assessed in duplicated radiometric assay containing 100uM [gamma-32P] ATP and quantified by p81 phosphocellulose assay.More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/1/2011
Entry Details Article
PubMed
TargetAurora kinase A(Mouse)
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataIC50: 4nMAssay Description:Inhibition of GST-tagged recombinant mouse Aurora A expressed in Sf9 cells using biotin-GLRRASLG as peptide substrate by [gamma-33S]ATP binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2015
Entry Details Article
PubMed
TargetAurora kinase A(Mouse)
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataIC50: 4nMAssay Description:Inhibition of recombinant mouse GST-tagged Aurora A expressed in insect Sf9 cells using Biotin-GLRRASLG as substrate in presence of [gamma33P]ATP by ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataIC50: 4nMAssay Description:Inhibition of Aurora AMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataIC50: 4nMAssay Description:Inhibition of Aurora A kinase (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMed
TargetAurora kinase A(Mouse)
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataIC50: 4nMAssay Description:Inhibition of recombinant mouse Aurora A kinase expressed in Sf9 cells using Biotin-GLRRASLG as substrate in presence of [gamma33]P-ATP by FlashPlate...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataIC50: 4nMAssay Description:Inhibition of aurora A kinaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/22/2012
Entry Details Article
PubMed
TargetAurora kinase A(Mouse)
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataIC50: 4nMAssay Description:Inhibition of mouse recombinant Aurora A kinase expressed in insect Sf9 cells by radioactive flashplate assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2012
Entry Details Article
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataIC50: 5nMAssay Description:Inhibition of human aurora AMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataIC50: 5nMT: 2°CAssay Description:Inhibition of Aurora A was assessed in duplicated radiometric assay containing 100uM [gamma-32P] ATP and quantified by p81 phosphocellulose assay.More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/1/2011
Entry Details Article
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataKd:  6.5nMAssay Description:Binding constant for AURKA kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataKd:  6.5nMAssay Description:Binding constant for AURKA kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/25/2012
Entry Details Article
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataKd:  6.5nMpH: 7.4 T: 2°CAssay Description:Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/14/2009
Entry Details
PCBioAssay
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM50277545(Alisertib | MLN8237 | CHEMBL483158 | 4-(9-chloro-7...)
Affinity DataIC50: 6.70nMAssay Description:Inhibition of Aurora A kinase autophosphorylation at Thr288 in human HeLa Kyoto cells incubated for 20 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/18/2018
Entry Details Article
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM50277545(Alisertib | MLN8237 | CHEMBL483158 | 4-(9-chloro-7...)
Affinity DataIC50: 7nMAssay Description:Inhibition of aurora kinase A autophosphorylation at T288 in human HCT116 cells by immunofluorescence analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/22/2016
Entry Details Article
PubMed
TargetAurora kinase A(Mouse)
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataKi:  7nMAssay Description:Competitive inhibition of recombinant mouse aurora kinase A expressed in insect Sf9 cells in presence of ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/22/2016
Entry Details Article
PubMed
TargetMAP kinase-activated protein kinase 5(Human)
Vertex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataKd:  8nMAssay Description:Binding affinity to PRAK2More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/22/2012
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase 17B(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataKd:  8.10nMAssay Description:Binding constant for DRAK2 kinase domainMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2012
Entry Details Article
PubMed
TargetSerine/threonine-protein kinase 17B(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataKd:  8.10nMAssay Description:Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2011
Entry Details
PCBioAssay
TargetSerine/threonine-protein kinase 17B(Human)
Ambit Biosciences

Curated by ChEMBL
LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataKd:  8.10nMAssay Description:Binding constant for full-length DRAK2More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/25/2012
Entry Details Article
PubMed
TargetAurora kinase C(Human)
Harvard Medical School

LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataIC50: 9.10nMAssay Description:In vitro kinase assay of Aurora A, B, and C using Z-LYTE technology (Invitrogen) and ATP at Km apparent for each kinase.More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/4/2012
Entry Details Article
PubMed
TargetAurora kinase B(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataIC50: 9.30nMpH: 7.5 T: 2°CAssay Description:Aurora kinase was assayed in ELISA format using a GST fusion of the N-terminus of Histone H3 as substrate. Plates were coated with substrate, and the...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/28/2009
Entry Details Article
PubMed
TargetAurora kinase A(Mouse)
Takeda Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50097413(CHEMBL3586473)
Affinity DataIC50: 10nMAssay Description:Inhibition of recombinant mouse aurora kinase A expressed in insect Sf9 cells using biotin-GLRRASLG as substrate in presence of [gamma-33P]ATPMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/22/2016
Entry Details Article
PubMed
TargetMAP kinase-interacting serine/threonine-protein kinase 2(Human)
Boehringer Ingelheim International

US Patent
LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataIC50: 13nMpH: 7.4 T: 2°CAssay Description:Inhibition of kinase activity of Mnk1 and Mnk2a was assessed with the same assay system, using pre-activated GST-Mnk1 or GST-Mnk2a, respectively. The...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/16/2015
Entry Details
Go to US Patent

TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM50277545(Alisertib | MLN8237 | CHEMBL483158 | 4-(9-chloro-7...)
Affinity DataIC50: 13nMAssay Description:Inhibition of recombinant GST-tagged N-terminal truncated human Aurora A (123 to 401 residues) expressed in Sf9 insect cell using tetra-LRRASLG pepti...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/5/2023
Entry Details Article
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM50277545(Alisertib | MLN8237 | CHEMBL483158 | 4-(9-chloro-7...)
Affinity DataIC50: 15nMAssay Description:Inhibition of Aurora A in human ANBL-6 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell prol...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetAurora kinase A(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM50097413(CHEMBL3586473)
Affinity DataIC50: 18nMAssay Description:Inhibition of aurora kinase A autophosphorylation at T288 in human HCT116 cells by immunofluorescence analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/22/2016
Entry Details Article
PubMed
TargetAurora kinase B(Human)
University of Berne

Curated by ChEMBL
LigandPNGBDBM31093(cid_11712649 | 4-[[7-[2,6-bis(fluoranyl)phenyl]-9-...)
Affinity DataIC50: 23.2nMAssay Description:In vitro kinase assay of Aurora A, B, and C using Z-LYTE technology (Invitrogen) and ATP at Km apparent for each kinase.More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/4/2012
Entry Details Article
PubMed
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