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PubMed code 22247788

Compile data set for download or QSAR
Found 40 hits of Enzyme Inhibition Constant Data   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM28031
PNG
(BMS-777607 | N-{4-[(2-amino-3-chloropyridin-4-yl)o...)
Show SMILES CCOc1ccn(-c2ccc(F)cc2)c(=O)c1C(=O)Nc1ccc(Oc2ccnc(N)c2Cl)c(F)c1
Show InChI InChI=1S/C25H19ClF2N4O4/c1-2-35-19-10-12-32(16-6-3-14(27)4-7-16)25(34)21(19)24(33)31-15-5-8-18(17(28)13-15)36-20-9-11-30-23(29)22(20)26/h3-13H,2H2,1H3,(H2,29,30)(H,31,33)
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n/an/a 1.10n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
Aurora kinase A


(Homo sapiens (human))
BDBM50382425
PNG
(CHEMBL2022968)
Show SMILES CN(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(CN3CCN(C)CC3)cc2)ncc1Cl
Show InChI InChI=1S/C24H30ClN7O2S/c1-30(2)35(33,34)22-7-5-4-6-21(22)28-23-20(25)16-26-24(29-23)27-19-10-8-18(9-11-19)17-32-14-12-31(3)13-15-32/h4-11,16H,12-15,17H2,1-3H3,(H2,26,27,28,29)
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n/an/a 3n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of Aurora A


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM27917
PNG
(4-cyano-N-[4-(4-methylpiperazin-1-yl)-2-(4-methylp...)
Show SMILES CC1CCN(CC1)c1cc(ccc1NC(=O)c1cc(c[nH]1)C#N)N1CCN(C)CC1
Show InChI InChI=1S/C23H30N6O/c1-17-5-7-29(8-6-17)22-14-19(28-11-9-27(2)10-12-28)3-4-20(22)26-23(30)21-13-18(15-24)16-25-21/h3-4,13-14,16-17,25H,5-12H2,1-2H3,(H,26,30)
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n/an/a 6.40n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
Aurora kinase B


(Homo sapiens (Human))
BDBM50382425
PNG
(CHEMBL2022968)
Show SMILES CN(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(CN3CCN(C)CC3)cc2)ncc1Cl
Show InChI InChI=1S/C24H30ClN7O2S/c1-30(2)35(33,34)22-7-5-4-6-21(22)28-23-20(25)16-26-24(29-23)27-19-10-8-18(9-11-19)17-32-14-12-31(3)13-15-32/h4-11,16H,12-15,17H2,1-3H3,(H2,26,27,28,29)
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n/an/a 12n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of Aurora B


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Mer


(Homo sapiens)
BDBM28031
PNG
(BMS-777607 | N-{4-[(2-amino-3-chloropyridin-4-yl)o...)
Show SMILES CCOc1ccn(-c2ccc(F)cc2)c(=O)c1C(=O)Nc1ccc(Oc2ccnc(N)c2Cl)c(F)c1
Show InChI InChI=1S/C25H19ClF2N4O4/c1-2-35-19-10-12-32(16-6-3-14(27)4-7-16)25(34)21(19)24(33)31-15-5-8-18(17(28)13-15)36-20-9-11-30-23(29)22(20)26/h3-13H,2H2,1H3,(H2,29,30)(H,31,33)
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n/an/a 14n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of Mer kinase


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382441
PNG
(CHEMBL2023349)
Show SMILES Nc1nc(Nc2ccc3CCC(CCc3c2)N2CCCC2)nn1-c1cc2CCCc3ccccc3-c2nn1
Show InChI InChI=1S/C30H34N8/c31-29-33-30(32-24-13-10-20-11-14-25(15-12-22(20)18-24)37-16-3-4-17-37)36-38(29)27-19-23-8-5-7-21-6-1-2-9-26(21)28(23)35-34-27/h1-2,6,9-10,13,18-19,25H,3-5,7-8,11-12,14-17H2,(H3,31,32,33,36)
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TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382443
PNG
(CHEMBL2023351)
Show SMILES COc1cc2c(Oc3cc(NS(=O)(=O)c4cc(F)ccc4F)ccc3F)ccnc2cc1OCCCN1CCC(C)CC1
Show InChI InChI=1S/C31H32F3N3O5S/c1-20-9-13-37(14-10-20)12-3-15-41-30-19-26-23(18-29(30)40-2)27(8-11-35-26)42-28-17-22(5-7-24(28)33)36-43(38,39)31-16-21(32)4-6-25(31)34/h4-8,11,16-20,36H,3,9-10,12-15H2,1-2H3
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TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382414
PNG
(CHEMBL2022975)
Show SMILES CN1CCN(Cc2ccc(Nc3ncc(Cl)c(Nc4ccccc4S(=O)(=O)N4CCCC4)n3)cc2)CC1
Show InChI InChI=1S/C26H32ClN7O2S/c1-32-14-16-33(17-15-32)19-20-8-10-21(11-9-20)29-26-28-18-22(27)25(31-26)30-23-6-2-3-7-24(23)37(35,36)34-12-4-5-13-34/h2-3,6-11,18H,4-5,12-17,19H2,1H3,(H2,28,29,30,31)
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TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382425
PNG
(CHEMBL2022968)
Show SMILES CN(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(CN3CCN(C)CC3)cc2)ncc1Cl
Show InChI InChI=1S/C24H30ClN7O2S/c1-30(2)35(33,34)22-7-5-4-6-21(22)28-23-20(25)16-26-24(29-23)27-19-10-8-18(9-11-19)17-32-14-12-31(3)13-15-32/h4-11,16H,12-15,17H2,1-3H3,(H2,26,27,28,29)
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TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382442
PNG
(CHEMBL2023350)
Show SMILES CN1CCC(CC1)n1cc(c(C)n1)-c1cnc(N)c(c1)-c1nc2ccccc2o1
Show InChI InChI=1S/C22H24N6O/c1-14-18(13-28(26-14)16-7-9-27(2)10-8-16)15-11-17(21(23)24-12-15)22-25-19-5-3-4-6-20(19)29-22/h3-6,11-13,16H,7-10H2,1-2H3,(H2,23,24)
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TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382431
PNG
(CHEMBL2022974)
Show SMILES CN1CCN(Cc2ccc(Nc3ncc(Cl)c(Nc4ccccc4C(=O)NC4CC4)n3)cc2)CC1
Show InChI InChI=1S/C26H30ClN7O/c1-33-12-14-34(15-13-33)17-18-6-8-20(9-7-18)30-26-28-16-22(27)24(32-26)31-23-5-3-2-4-21(23)25(35)29-19-10-11-19/h2-9,16,19H,10-15,17H2,1H3,(H,29,35)(H2,28,30,31,32)
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TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382433
PNG
(CHEMBL2022977)
Show SMILES CN1CCN(Cc2ccc(Nc3ncc(Cl)c(Nc4ccc(F)cc4S(=O)(=O)N4CCCC4)n3)cc2)CC1
Show InChI InChI=1S/C26H31ClFN7O2S/c1-33-12-14-34(15-13-33)18-19-4-7-21(8-5-19)30-26-29-17-22(27)25(32-26)31-23-9-6-20(28)16-24(23)38(36,37)35-10-2-3-11-35/h4-9,16-17H,2-3,10-15,18H2,1H3,(H2,29,30,31,32)
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TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382439
PNG
(CHEMBL2023347)
Show SMILES CN(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(cc2)N(C)C2CCN(C)CC2)ncc1Cl
Show InChI InChI=1S/C25H32ClN7O2S/c1-31(2)36(34,35)23-8-6-5-7-22(23)29-24-21(26)17-27-25(30-24)28-18-9-11-19(12-10-18)33(4)20-13-15-32(3)16-14-20/h5-12,17,20H,13-16H2,1-4H3,(H2,27,28,29,30)
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TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382430
PNG
(CHEMBL2022973)
Show SMILES CN1CCN(Cc2ccc(Nc3ncc(Cl)c(Nc4ccccc4C(=O)N4CCCC4)n3)cc2)CC1
Show InChI InChI=1S/C27H32ClN7O/c1-33-14-16-34(17-15-33)19-20-8-10-21(11-9-20)30-27-29-18-23(28)25(32-27)31-24-7-3-2-6-22(24)26(36)35-12-4-5-13-35/h2-3,6-11,18H,4-5,12-17,19H2,1H3,(H2,29,30,31,32)
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TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382437
PNG
(CHEMBL2023345)
Show SMILES CN(C)S(=O)(=O)c1cc(F)ccc1-c1nc(Nc2ccc(CN3CCN(C)CC3)cc2)ncc1Cl
Show InChI InChI=1S/C24H28ClFN6O2S/c1-30(2)35(33,34)22-14-18(26)6-9-20(22)23-21(25)15-27-24(29-23)28-19-7-4-17(5-8-19)16-32-12-10-31(3)11-13-32/h4-9,14-15H,10-13,16H2,1-3H3,(H,27,28,29)
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TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382426
PNG
(CHEMBL2022969)
Show SMILES CN(C)C(=O)c1ccccc1Nc1nc(Nc2ccc(CN3CCN(C)CC3)cc2)ncc1Cl
Show InChI InChI=1S/C25H30ClN7O/c1-31(2)24(34)20-6-4-5-7-22(20)29-23-21(26)16-27-25(30-23)28-19-10-8-18(9-11-19)17-33-14-12-32(3)13-15-33/h4-11,16H,12-15,17H2,1-3H3,(H2,27,28,29,30)
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TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382438
PNG
(CHEMBL2023346)
Show SMILES CN1CCN(Cc2ccc(Nc3ncc(Cl)c(n3)-c3ccc(F)cc3S(=O)(=O)N3CCCC3)cc2)CC1
Show InChI InChI=1S/C26H30ClFN6O2S/c1-32-12-14-33(15-13-32)18-19-4-7-21(8-5-19)30-26-29-17-23(27)25(31-26)22-9-6-20(28)16-24(22)37(35,36)34-10-2-3-11-34/h4-9,16-17H,2-3,10-15,18H2,1H3,(H,29,30,31)
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TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382444
PNG
(CHEMBL2023352)
Show SMILES Cc1c[nH]c2nc(Nc3ccc(cc3)N3CCN(CCO)CC3)nc(-c3cccc(CC#N)c3)c12
Show InChI InChI=1S/C27H29N7O/c1-19-18-29-26-24(19)25(21-4-2-3-20(17-21)9-10-28)31-27(32-26)30-22-5-7-23(8-6-22)34-13-11-33(12-14-34)15-16-35/h2-8,17-18,35H,9,11-16H2,1H3,(H2,29,30,31,32)
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TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382432
PNG
(CHEMBL2022976)
Show SMILES CN1CCN(Cc2ccc(Nc3ncc(Cl)c(Nc4ccc(F)cc4S(=O)(=O)N4CCOCC4)n3)cc2)CC1
Show InChI InChI=1S/C26H31ClFN7O3S/c1-33-8-10-34(11-9-33)18-19-2-5-21(6-3-19)30-26-29-17-22(27)25(32-26)31-23-7-4-20(28)16-24(23)39(36,37)35-12-14-38-15-13-35/h2-7,16-17H,8-15,18H2,1H3,(H2,29,30,31,32)
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TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382421
PNG
(CHEMBL2022964)
Show SMILES CN1CCN(Cc2ccc(Nc3ncc(C)c(n3)-c3ccc(cc3)C(C)(C)C#N)cc2)CC1
Show InChI InChI=1S/C27H32N6/c1-20-17-29-26(31-25(20)22-7-9-23(10-8-22)27(2,3)19-28)30-24-11-5-21(6-12-24)18-33-15-13-32(4)14-16-33/h5-12,17H,13-16,18H2,1-4H3,(H,29,30,31)
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n/an/a 290n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50306682
PNG
((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Show SMILES C[C@@H](Oc1cc(cnc1N)-c1cnn(c1)C1CCNCC1)c1c(Cl)ccc(F)c1Cl
Show InChI InChI=1S/C21H22Cl2FN5O/c1-12(19-16(22)2-3-17(24)20(19)23)30-18-8-13(9-27-21(18)25)14-10-28-29(11-14)15-4-6-26-7-5-15/h2-3,8-12,15,26H,4-7H2,1H3,(H2,25,27)/t12-/m1/s1
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n/an/a 300n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382419
PNG
(CHEMBL2022962)
Show SMILES CN(C1CCN(C)CC1)c1ccc(Nc2ncc(C)c(n2)-c2ccc(F)c(Cl)c2)cc1
Show InChI InChI=1S/C24H27ClFN5/c1-16-15-27-24(29-23(16)17-4-9-22(26)21(25)14-17)28-18-5-7-19(8-6-18)31(3)20-10-12-30(2)13-11-20/h4-9,14-15,20H,10-13H2,1-3H3,(H,27,28,29)
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n/an/a 420n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382420
PNG
(CHEMBL2022963)
Show SMILES CN1CCN(Cc2ccc(Nc3ncc(C)c(n3)-c3cccc(Cl)c3)cc2)CC1
Show InChI InChI=1S/C23H26ClN5/c1-17-15-25-23(27-22(17)19-4-3-5-20(24)14-19)26-21-8-6-18(7-9-21)16-29-12-10-28(2)11-13-29/h3-9,14-15H,10-13,16H2,1-2H3,(H,25,26,27)
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n/an/a 440n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382417
PNG
(CHEMBL2022575)
Show SMILES CN1CCN(Cc2ccc(Nc3ncc(C)c(n3)-c3ccc(F)c(Cl)c3)cc2)CC1
Show InChI InChI=1S/C23H25ClFN5/c1-16-14-26-23(28-22(16)18-5-8-21(25)20(24)13-18)27-19-6-3-17(4-7-19)15-30-11-9-29(2)10-12-30/h3-8,13-14H,9-12,15H2,1-2H3,(H,26,27,28)
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n/an/a 730n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382434
PNG
(CHEMBL2022978)
Show SMILES CN1CCN(Cc2ccc(Nc3ncc(Cl)c(Nc4ccc(Cl)cc4S(=O)(=O)N4CCCC4)n3)cc2)CC1
Show InChI InChI=1S/C26H31Cl2N7O2S/c1-33-12-14-34(15-13-33)18-19-4-7-21(8-5-19)30-26-29-17-22(28)25(32-26)31-23-9-6-20(27)16-24(23)38(36,37)35-10-2-3-11-35/h4-9,16-17H,2-3,10-15,18H2,1H3,(H2,29,30,31,32)
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n/an/a 1.08E+3n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382428
PNG
(CHEMBL2022971)
Show SMILES CN1CCN(Cc2ccc(Nc3ncc(F)c(n3)-c3ccc(F)cc3S(=O)(=O)N3CCCC3)cc2)CC1
Show InChI InChI=1S/C26H30F2N6O2S/c1-32-12-14-33(15-13-32)18-19-4-7-21(8-5-19)30-26-29-17-23(28)25(31-26)22-9-6-20(27)16-24(22)37(35,36)34-10-2-3-11-34/h4-9,16-17H,2-3,10-15,18H2,1H3,(H,29,30,31)
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n/an/a 1.15E+3n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382435
PNG
(CHEMBL2023343)
Show SMILES CN1CCN(Cc2ccc(Nc3ncc(Cl)c(Nc4ccc(O)cc4S(=O)(=O)N4CCCC4)n3)cc2)CC1
Show InChI InChI=1S/C26H32ClN7O3S/c1-32-12-14-33(15-13-32)18-19-4-6-20(7-5-19)29-26-28-17-22(27)25(31-26)30-23-9-8-21(35)16-24(23)38(36,37)34-10-2-3-11-34/h4-9,16-17,35H,2-3,10-15,18H2,1H3,(H2,28,29,30,31)
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n/an/a 1.32E+3n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382422
PNG
(CHEMBL2022965)
Show SMILES CN1CCN(Cc2ccc(Nc3ncc(C)c(Oc4ccc(F)c(Cl)c4)n3)cc2)CC1
Show InChI InChI=1S/C23H25ClFN5O/c1-16-14-26-23(28-22(16)31-19-7-8-21(25)20(24)13-19)27-18-5-3-17(4-6-18)15-30-11-9-29(2)10-12-30/h3-8,13-14H,9-12,15H2,1-2H3,(H,26,27,28)
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n/an/a 1.40E+3n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382418
PNG
(CHEMBL2022961)
Show SMILES Cc1cnc(Nc2ccc(OCCN3CCCCC3)cc2)nc1-c1ccc(F)c(Cl)c1
Show InChI InChI=1S/C24H26ClFN4O/c1-17-16-27-24(29-23(17)18-5-10-22(26)21(25)15-18)28-19-6-8-20(9-7-19)31-14-13-30-11-3-2-4-12-30/h5-10,15-16H,2-4,11-14H2,1H3,(H,27,28,29)
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n/an/a 1.63E+3n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382440
PNG
(CHEMBL2023348)
Show SMILES CN(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(cc2)N2CCN(C)CC2)ncc1Cl
Show InChI InChI=1S/C23H28ClN7O2S/c1-29(2)34(32,33)21-7-5-4-6-20(21)27-22-19(24)16-25-23(28-22)26-17-8-10-18(11-9-17)31-14-12-30(3)13-15-31/h4-11,16H,12-15H2,1-3H3,(H2,25,26,27,28)
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n/an/a 1.73E+3n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382415
PNG
(CHEMBL2022573)
Show SMILES CN1CCN(CC1)c1ccc(Nc2ncc(C)c(n2)-c2ccc(F)c(Cl)c2)cc1F
Show InChI InChI=1S/C22H22ClF2N5/c1-14-13-26-22(28-21(14)15-3-5-18(24)17(23)11-15)27-16-4-6-20(19(25)12-16)30-9-7-29(2)8-10-30/h3-6,11-13H,7-10H2,1-2H3,(H,26,27,28)
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n/an/a 2.80E+3n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382427
PNG
(CHEMBL2022970)
Show SMILES CN1CCN(Cc2ccc(Nc3ncc(C)c(n3)-c3ccc(F)cc3S(=O)(=O)N3CCCC3)cc2)CC1
Show InChI InChI=1S/C27H33FN6O2S/c1-20-18-29-27(30-23-8-5-21(6-9-23)19-33-15-13-32(2)14-16-33)31-26(20)24-10-7-22(28)17-25(24)37(35,36)34-11-3-4-12-34/h5-10,17-18H,3-4,11-16,19H2,1-2H3,(H,29,30,31)
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n/an/a 2.93E+3n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382424
PNG
(CHEMBL2022967)
Show SMILES CN1CCN(Cc2ccc(Nc3ncc(C4CC4)c(n3)-c3ccc(F)c(Cl)c3)cc2)CC1
Show InChI InChI=1S/C25H27ClFN5/c1-31-10-12-32(13-11-31)16-17-2-7-20(8-3-17)29-25-28-15-21(18-4-5-18)24(30-25)19-6-9-23(27)22(26)14-19/h2-3,6-9,14-15,18H,4-5,10-13,16H2,1H3,(H,28,29,30)
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n/an/a 3.40E+3n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382436
PNG
(CHEMBL2023344)
Show SMILES CN(c1ccc(F)cc1S(=O)(=O)N1CCCC1)c1nc(Nc2ccc(CN3CCN(C)CC3)cc2)ncc1Cl
Show InChI InChI=1S/C27H33ClFN7O2S/c1-33-13-15-35(16-14-33)19-20-5-8-22(9-6-20)31-27-30-18-23(28)26(32-27)34(2)24-10-7-21(29)17-25(24)39(37,38)36-11-3-4-12-36/h5-10,17-18H,3-4,11-16,19H2,1-2H3,(H,30,31,32)
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n/an/a 3.91E+3n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382416
PNG
(CHEMBL2022574)
Show SMILES CN1CCN(CC1)c1ccc(Nc2ncc(C)c(n2)-c2ccc(F)cc2)cc1F
Show InChI InChI=1S/C22H23F2N5/c1-15-14-25-22(27-21(15)16-3-5-17(23)6-4-16)26-18-7-8-20(19(24)13-18)29-11-9-28(2)10-12-29/h3-8,13-14H,9-12H2,1-2H3,(H,25,26,27)
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n/an/a 6.10E+3n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382429
PNG
(CHEMBL2022972)
Show SMILES CN(C)C(=O)c1ccccc1Nc1nc(Nc2ccc(CN3CCN(C)CC3)cc2)ncc1C(F)(F)F
Show InChI InChI=1S/C26H30F3N7O/c1-34(2)24(37)20-6-4-5-7-22(20)32-23-21(26(27,28)29)16-30-25(33-23)31-19-10-8-18(9-11-19)17-36-14-12-35(3)13-15-36/h4-11,16H,12-15,17H2,1-3H3,(H2,30,31,32,33)
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n/an/a>1.00E+4n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
Tyrosine-protein kinase Mer


(Homo sapiens)
BDBM50113707
PNG
(2,6,9-Trisubstitute purine, 2 | 2-(2-hydroxyethyla...)
Show SMILES CC(C)n1cnc2c(Nc3cccc(Cl)c3)nc(NCCO)nc12
Show InChI InChI=1S/C16H19ClN6O/c1-10(2)23-9-19-13-14(20-12-5-3-4-11(17)8-12)21-16(18-6-7-24)22-15(13)23/h3-5,8-10,24H,6-7H2,1-2H3,(H2,18,20,21,22)
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n/an/a 1.13E+4n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of Mer kinase


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382423
PNG
(CHEMBL2022966)
Show SMILES CN1CCN(Cc2ccc(Nc3ncc(C)c(Nc4ccc(F)c(Cl)c4)n3)cc2)CC1
Show InChI InChI=1S/C23H26ClFN6/c1-16-14-26-23(29-22(16)27-19-7-8-21(25)20(24)13-19)28-18-5-3-17(4-6-18)15-31-11-9-30(2)10-12-31/h3-8,13-14H,9-12,15H2,1-2H3,(H2,26,27,28,29)
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n/an/a 6.27E+4n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382425
PNG
(CHEMBL2022968)
Show SMILES CN(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(CN3CCN(C)CC3)cc2)ncc1Cl
Show InChI InChI=1S/C24H30ClN7O2S/c1-30(2)35(33,34)22-7-5-4-6-21(22)28-23-20(25)16-26-24(29-23)27-19-10-8-18(9-11-19)17-32-14-12-31(3)13-15-32/h4-11,16H,12-15,17H2,1-3H3,(H2,26,27,28,29)
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n/an/an/an/a 222n/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of AXL in human PSN1 cells assessed as decrease in GAS6-induced phospho-AXL level after 2 hrs by EILSA


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
AXL receptor tyrosine kinase


(Homo sapiens (Human))
BDBM50382425
PNG
(CHEMBL2022968)
Show SMILES CN(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(CN3CCN(C)CC3)cc2)ncc1Cl
Show InChI InChI=1S/C24H30ClN7O2S/c1-30(2)35(33,34)22-7-5-4-6-21(22)28-23-20(25)16-26-24(29-23)27-19-10-8-18(9-11-19)17-32-14-12-31(3)13-15-32/h4-11,16H,12-15,17H2,1-3H3,(H2,26,27,28,29)
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KEGG

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UniChem

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Article
PubMed
n/an/an/an/a 305n/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of AXL-mediated AKT Ser473 phosphorylation in human PSN1 cells assessed as decrease in GAS6-induced phospho-AKT level after 2 hrs by ELISA


ACS Med Chem Lett 2: 907-912 (2011)


Article DOI: 10.1021/ml200198x
BindingDB Entry DOI: 10.7270/Q2DZ099R
More data for this
Ligand-Target Pair
* indicates data uncertainty>20%