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Compile Data Set for Download or QSAR

Found 1098 hits of ic50 for UniProtKB: P16234   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kcal/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50191945
PNG
(CHEMBL3904768)
Show SMILES Cn1nccc1-c1ccn2c(cnc2c1)C(=O)Nc1cc(ccc1F)C(=O)NCc1ccc(F)c(F)c1
Show InChI InChI=1S/C26H19F3N6O2/c1-34-22(6-8-32-34)16-7-9-35-23(14-30-24(35)12-16)26(37)33-21-11-17(3-5-19(21)28)25(36)31-13-15-2-4-18(27)20(29)10-15/h2-12,14H,13H2,1H3,(H,31,36)(H,33,37)
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n/an/a 0.0900n/an/an/an/an/an/a



Novartis Institutes of Biomedical Research (NIBR)

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha kinase domain (unknown origin) assessed as reduction in probe peptide substrate phosphorylation by capillary electrophoresis


J Med Chem 59: 7901-14 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00703
BindingDB Entry DOI: 10.7270/Q25X2BW1
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM2579
PNG
((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Show SMILES CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r|
Show InChI InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1
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n/an/a<0.100n/an/an/an/an/an/a



National Cancer Institute

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha


J Med Chem 52: 3191-204 (2009)


Article DOI: 10.1021/jm800861c
BindingDB Entry DOI: 10.7270/Q23J3DWT
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50191977
PNG
(CHEMBL3983564)
Show SMILES CN1CCN(CC1)c1ccccc1CNC(=O)c1ccc(F)c(NC(=O)c2cnc3cc(ccn23)-c2cc[nH]n2)c1
Show InChI InChI=1S/C30H29FN8O2/c1-37-12-14-38(15-13-37)26-5-3-2-4-22(26)18-33-29(40)21-6-7-23(31)25(16-21)35-30(41)27-19-32-28-17-20(9-11-39(27)28)24-8-10-34-36-24/h2-11,16-17,19H,12-15,18H2,1H3,(H,33,40)(H,34,36)(H,35,41)
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n/an/a<0.100n/an/an/an/an/an/a



Novartis Institutes of Biomedical Research (NIBR)

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha kinase domain (unknown origin) assessed as reduction in probe peptide substrate phosphorylation by capillary electrophoresis


J Med Chem 59: 7901-14 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00703
BindingDB Entry DOI: 10.7270/Q25X2BW1
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50191981
PNG
(CHEMBL3979322)
Show SMILES CN1CCN(CC1)c1ccccc1CNC(=O)c1ccc(F)c(NC(=O)c2cnc3cc(ccn23)-c2ccnn2C)c1
Show InChI InChI=1S/C31H31FN8O2/c1-37-13-15-39(16-14-37)27-6-4-3-5-23(27)19-34-30(41)22-7-8-24(32)25(17-22)36-31(42)28-20-33-29-18-21(10-12-40(28)29)26-9-11-35-38(26)2/h3-12,17-18,20H,13-16,19H2,1-2H3,(H,34,41)(H,36,42)
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n/an/a 0.180n/an/an/an/an/an/a



Novartis Institutes of Biomedical Research (NIBR)

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha kinase domain (unknown origin) assessed as reduction in probe peptide substrate phosphorylation by capillary electrophoresis


J Med Chem 59: 7901-14 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00703
BindingDB Entry DOI: 10.7270/Q25X2BW1
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50191973
PNG
(CHEMBL3940697)
Show SMILES Cn1cc(cn1)-c1ccn2c(cnc2c1)C(=O)Nc1cc(ccc1F)C(=O)NCCN1CCCC1(C)C
Show InChI InChI=1S/C27H30FN7O2/c1-27(2)8-4-10-34(27)12-9-29-25(36)19-5-6-21(28)22(13-19)32-26(37)23-16-30-24-14-18(7-11-35(23)24)20-15-31-33(3)17-20/h5-7,11,13-17H,4,8-10,12H2,1-3H3,(H,29,36)(H,32,37)
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n/an/a 0.190n/an/an/an/an/an/a



Novartis Institutes of Biomedical Research (NIBR)

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha kinase domain (unknown origin) assessed as reduction in probe peptide substrate phosphorylation by capillary electrophoresis


J Med Chem 59: 7901-14 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00703
BindingDB Entry DOI: 10.7270/Q25X2BW1
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50191978
PNG
(CHEMBL3915941)
Show SMILES Cc1ncc(cc1NC(=O)c1cnn2cc(ccc12)-c1cnn(C)c1)C(=O)NCCN1CCCC1(C)C
Show InChI InChI=1S/C27H32N8O2/c1-18-23(12-20(13-29-18)25(36)28-9-11-34-10-5-8-27(34,2)3)32-26(37)22-15-31-35-17-19(6-7-24(22)35)21-14-30-33(4)16-21/h6-7,12-17H,5,8-11H2,1-4H3,(H,28,36)(H,32,37)
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n/an/a 0.200n/an/an/an/an/an/a



Novartis Institutes of Biomedical Research (NIBR)

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha kinase domain (unknown origin) assessed as reduction in probe peptide substrate phosphorylation by capillary electrophoresis


J Med Chem 59: 7901-14 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00703
BindingDB Entry DOI: 10.7270/Q25X2BW1
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50336457
PNG
((3S,5Z,8S,9R,11E)-8,9,16-trihydroxy-14-methoxy-3-m...)
Show SMILES COc1cc(O)c2c(CCCC(=O)C(=O)C(=O)CCC[C@H](C)OC2=O)c1 |r|
Show InChI InChI=1S/C19H22O7/c1-11-5-3-7-14(20)18(23)15(21)8-4-6-12-9-13(25-2)10-16(22)17(12)19(24)26-11/h9-11,22H,3-8H2,1-2H3/t11-/m0/s1
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n/an/a 0.240n/an/an/an/an/an/a



National University of Ireland

Curated by ChEMBL


Assay Description
Inhibition of human recombinant PDGFRalpha in cell free system after 60 mins


Bioorg Med Chem Lett 21: 1167-70 (2011)


Article DOI: 10.1016/j.bmcl.2010.12.100
BindingDB Entry DOI: 10.7270/Q23T9HH5
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50191974
PNG
(CHEMBL3913766)
Show SMILES CN1CCN(CC1)c1ccccc1CNC(=O)c1ccc(F)c(NC(=O)c2cnc3cc(ccn23)-c2cnn(C)c2)c1
Show InChI InChI=1S/C31H31FN8O2/c1-37-11-13-39(14-12-37)27-6-4-3-5-23(27)17-34-30(41)22-7-8-25(32)26(15-22)36-31(42)28-19-33-29-16-21(9-10-40(28)29)24-18-35-38(2)20-24/h3-10,15-16,18-20H,11-14,17H2,1-2H3,(H,34,41)(H,36,42)
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n/an/a 0.320n/an/an/an/an/an/a



Novartis Institutes of Biomedical Research (NIBR)

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha kinase domain (unknown origin) assessed as reduction in probe peptide substrate phosphorylation by capillary electrophoresis


J Med Chem 59: 7901-14 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00703
BindingDB Entry DOI: 10.7270/Q25X2BW1
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM2579
PNG
((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Show SMILES CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r|
Show InChI InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1
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n/an/a 0.418n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of human PDGFRalpha using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay


Citation and Details

Article DOI: 10.1016/j.bmc.2018.02.022
BindingDB Entry DOI: 10.7270/Q2DJ5KB8
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM2579
PNG
((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Show SMILES CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r|
Show InChI InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1
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n/an/a 0.430n/an/an/an/an/an/a



Hangzhou Xixi Hospital

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha (unknown origin) by HTRF method


Bioorg Med Chem 25: 3195-3205 (2017)


Article DOI: 10.1016/j.bmc.2017.04.003
BindingDB Entry DOI: 10.7270/Q27P91JP
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM2579
PNG
((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Show SMILES CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r|
Show InChI InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1
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n/an/a 0.450n/an/an/an/an/an/a



Korea Institute of Science and Technology (KIST)

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha (unknown origin)


Eur J Med Chem 141: 657-675 (2017)


Article DOI: 10.1016/j.ejmech.2017.10.003
BindingDB Entry DOI: 10.7270/Q2CV4M86
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50191975
PNG
(CHEMBL3975580)
Show SMILES Cn1nccc1-c1ccn2c(cnc2c1)C(=O)Nc1cc(ccc1F)C(=O)NCC1CCC(C)(C)O1
Show InChI InChI=1S/C26H27FN6O3/c1-26(2)9-6-18(36-26)14-29-24(34)17-4-5-19(27)20(12-17)31-25(35)22-15-28-23-13-16(8-11-33(22)23)21-7-10-30-32(21)3/h4-5,7-8,10-13,15,18H,6,9,14H2,1-3H3,(H,29,34)(H,31,35)
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n/an/a 0.530n/an/an/an/an/an/a



Novartis Institutes of Biomedical Research (NIBR)

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha kinase domain (unknown origin) assessed as reduction in probe peptide substrate phosphorylation by capillary electrophoresis


J Med Chem 59: 7901-14 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00703
BindingDB Entry DOI: 10.7270/Q25X2BW1
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM2579
PNG
((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Show SMILES CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r|
Show InChI InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1
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n/an/a 0.580n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of PDGFRA (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition measured after 6...


Citation and Details

Article DOI: 10.1016/j.ejmech.2021.113327
BindingDB Entry DOI: 10.7270/Q2KP85X0
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM2579
PNG
((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Show SMILES CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r|
Show InChI InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1
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n/an/a 0.600n/an/an/an/an/an/a



Southeast University

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha (unknown origin) incubated for 1 hr by spectrophotometric analysis


Bioorg Med Chem 24: 3483-93 (2016)


Article DOI: 10.1016/j.bmc.2016.05.057
BindingDB Entry DOI: 10.7270/Q29G5PQT
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM106562
PNG
(US8586600, III-14)
Show SMILES Cc1ccc(cc1Nc1nccc(n1)-c1cccnc1)C(=O)Nc1ccc(NC(=O)CCl)c(c1)C(F)(F)F
Show InChI InChI=1S/C26H20ClF3N6O2/c1-15-4-5-16(11-22(15)36-25-32-10-8-20(35-25)17-3-2-9-31-14-17)24(38)33-18-6-7-21(34-23(37)13-27)19(12-18)26(28,29)30/h2-12,14H,13H2,1H3,(H,33,38)(H,34,37)(H,32,35,36)
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US Patent
n/an/a 0.730n/an/an/an/an/an/a



Celgene Avilomics Research, Inc.

US Patent


Assay Description
Compounds may also be assayed as inhibitors of PDGFR in a manner substantially similar to the method described in Roberts, et al., “Antiangiogen...


US Patent US8586600 (2013)


BindingDB Entry DOI: 10.7270/Q2M61HWH
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50191946
PNG
(CHEMBL3950278)
Show SMILES CN1CCN(CC1)c1ccccc1CNC(=O)c1ccc(F)c(NC(=O)c2cnc3cc(ccn23)-c2cccnc2)c1
Show InChI InChI=1S/C32H30FN7O2/c1-38-13-15-39(16-14-38)28-7-3-2-5-25(28)20-36-31(41)23-8-9-26(33)27(17-23)37-32(42)29-21-35-30-18-22(10-12-40(29)30)24-6-4-11-34-19-24/h2-12,17-19,21H,13-16,20H2,1H3,(H,36,41)(H,37,42)
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n/an/a 0.75n/an/an/an/an/an/a



Novartis Institutes of Biomedical Research (NIBR)

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha kinase domain (unknown origin) assessed as reduction in probe peptide substrate phosphorylation by capillary electrophoresis


J Med Chem 59: 7901-14 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00703
BindingDB Entry DOI: 10.7270/Q25X2BW1
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM2579
PNG
((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Show SMILES CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r|
Show InChI InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1
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n/an/a 0.793n/an/an/an/an/an/a



University of Florida

Curated by ChEMBL


Assay Description
Inhibition of human PDGFRalpha using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay


Eur J Med Chem 161: 456-467 (2019)


Article DOI: 10.1016/j.ejmech.2018.10.052
BindingDB Entry DOI: 10.7270/Q2W380MT
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50191980
PNG
(CHEMBL3985689)
Show SMILES CN1CCN(CC1)c1ccccc1CNC(=O)c1cnc(C)c(NC(=O)c2cnn3cc(ccc23)-c2ccnn2C)c1
Show InChI InChI=1S/C31H33N9O2/c1-21-26(36-31(42)25-19-35-40-20-23(8-9-29(25)40)27-10-11-34-38(27)3)16-24(18-32-21)30(41)33-17-22-6-4-5-7-28(22)39-14-12-37(2)13-15-39/h4-11,16,18-20H,12-15,17H2,1-3H3,(H,33,41)(H,36,42)
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n/an/a 0.960n/an/an/an/an/an/a



Novartis Institutes of Biomedical Research (NIBR)

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha kinase domain (unknown origin) assessed as reduction in probe peptide substrate phosphorylation by capillary electrophoresis


J Med Chem 59: 7901-14 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00703
BindingDB Entry DOI: 10.7270/Q25X2BW1
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50321892
PNG
((Z)-5-{6-[3-(4-Methoxyphenyl)-ureido]-2-oxo-1,2-di...)
Show SMILES COc1ccc(NC(=O)Nc2ccc3\C(=C\c4[nH]cc(C(O)=O)c4C)C(=O)Nc3c2)cc1
Show InChI InChI=1S/C23H20N4O5/c1-12-18(22(29)30)11-24-19(12)10-17-16-8-5-14(9-20(16)27-21(17)28)26-23(31)25-13-3-6-15(32-2)7-4-13/h3-11,24H,1-2H3,(H,27,28)(H,29,30)(H2,25,26,31)/b17-10-
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n/an/a 0.980n/an/an/an/an/an/a



National Taiwan University

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha


Bioorg Med Chem 18: 4674-86 (2011)


Article DOI: 10.1016/j.bmc.2010.05.021
BindingDB Entry DOI: 10.7270/Q2QF8TVS
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50051941
PNG
(CHEMBL3322565)
Show SMILES COc1ccc(NC(=O)CC(=O)Nc2ccc3\C(=C\c4[nH]c(C)c(C(O)=O)c4C)C(=O)Nc3c2)cc1
Show InChI InChI=1S/C26H24N4O6/c1-13-20(27-14(2)24(13)26(34)35)11-19-18-9-6-16(10-21(18)30-25(19)33)29-23(32)12-22(31)28-15-4-7-17(36-3)8-5-15/h4-11,27H,12H2,1-3H3,(H,28,31)(H,29,32)(H,30,33)(H,34,35)/b19-11-
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n/an/a<1n/an/an/an/an/an/a



National Taiwan University

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha (unknown origin) using EAIYAAPFAKKK substrate by radioisotope-based P81 filter-binding assay


Eur J Med Chem 84: 312-34 (2014)


Article DOI: 10.1016/j.ejmech.2014.07.033
BindingDB Entry DOI: 10.7270/Q2RV0QB7
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50389975
PNG
(CHEMBL2071201)
Show SMILES Cn1cc(Nc2ncc(Br)c(N[C@@H]3[C@@H]4C[C@@H](C=C4)[C@@H]3C(N)=O)n2)cn1 |r,c:16|
Show InChI InChI=1S/C16H18BrN7O/c1-24-7-10(5-20-24)21-16-19-6-11(17)15(23-16)22-13-9-3-2-8(4-9)12(13)14(18)25/h2-3,5-9,12-13H,4H2,1H3,(H2,18,25)(H2,19,21,22,23)/t8-,9+,12+,13-/m1/s1
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n/an/a 1n/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha by TR-FRET analysis


Bioorg Med Chem Lett 22: 4750-5 (2012)


Article DOI: 10.1016/j.bmcl.2012.05.067
BindingDB Entry DOI: 10.7270/Q20C4WTF
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50459416
PNG
(CHEMBL4216473)
Show SMILES COCCOc1cc(F)c2c(Nc3ccc(NC(=O)Cn4cc(nn4)C(C)C)cc3)ncnc2c1
Show InChI InChI=1S/C24H26FN7O3/c1-15(2)21-12-32(31-30-21)13-22(33)28-16-4-6-17(7-5-16)29-24-23-19(25)10-18(35-9-8-34-3)11-20(23)26-14-27-24/h4-7,10-12,14-15H,8-9,13H2,1-3H3,(H,28,33)(H,26,27,29)
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TBA



Citation and Details
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50051957
PNG
(CHEMBL3322566)
Show SMILES COc1ccc(NC(=O)CC(=O)Nc2ccc3\C(=C\c4[nH]c(C)c(C(=O)NCCN5CCCC5)c4C)C(=O)Nc3c2)cc1
Show InChI InChI=1S/C32H36N6O5/c1-19-26(34-20(2)30(19)32(42)33-12-15-38-13-4-5-14-38)17-25-24-11-8-22(16-27(24)37-31(25)41)36-29(40)18-28(39)35-21-6-9-23(43-3)10-7-21/h6-11,16-17,34H,4-5,12-15,18H2,1-3H3,(H,33,42)(H,35,39)(H,36,40)(H,37,41)/b25-17-
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n/an/a<1n/an/an/an/an/an/a



National Taiwan University

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha (unknown origin) using EAIYAAPFAKKK substrate by radioisotope-based P81 filter-binding assay


Eur J Med Chem 84: 312-34 (2014)


Article DOI: 10.1016/j.ejmech.2014.07.033
BindingDB Entry DOI: 10.7270/Q2RV0QB7
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50322535
PNG
(3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N...)
Show SMILES CN1CCN(Cc2ccc(NC(=O)c3ccc(C)c(c3)C#Cc3cnc4cccnn34)cc2C(F)(F)F)CC1
Show InChI InChI=1S/C29H27F3N6O/c1-20-5-6-22(16-21(20)8-10-25-18-33-27-4-3-11-34-38(25)27)28(39)35-24-9-7-23(26(17-24)29(30,31)32)19-37-14-12-36(2)13-15-37/h3-7,9,11,16-18H,12-15,19H2,1-2H3,(H,35,39)
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n/an/a 1.10n/an/an/an/an/an/a


TBA

Assay Description
Binding affinity to human PDGFRalpha using poly[Glu:Tyr] (4:1) as substrate by radiometric hotspot kinase assay


Citation and Details

Article DOI: 10.1021/acsmedchemlett.8b00081
BindingDB Entry DOI: 10.7270/Q2WM1J37
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50322535
PNG
(3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N...)
Show SMILES CN1CCN(Cc2ccc(NC(=O)c3ccc(C)c(c3)C#Cc3cnc4cccnn34)cc2C(F)(F)F)CC1
Show InChI InChI=1S/C29H27F3N6O/c1-20-5-6-22(16-21(20)8-10-25-18-33-27-4-3-11-34-38(25)27)28(39)35-24-9-7-23(26(17-24)29(30,31)32)19-37-14-12-36(2)13-15-37/h3-7,9,11,16-18H,12-15,19H2,1-2H3,(H,35,39)
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n/an/a 1.10n/an/an/an/an/an/a


TBA



Citation and Details

Article DOI: 10.1016/j.ejmech.2022.114442
BindingDB Entry DOI: 10.7270/Q2Z89HCM
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50601440
PNG
(CHEMBL5176837)
Show SMILES COc1cc2ncc(-c3cccc(NC4CCNC4)n3)n2cc1-c1cnn(C)c1
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n/an/a 1.10n/an/an/an/an/an/a


TBA



Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c01851
BindingDB Entry DOI: 10.7270/Q25Q515Z
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50431812
PNG
(CHEMBL2347053)
Show SMILES [O-][N+](=O)c1ccccc1-c1n[nH]cc1C=C1C(=O)Nc2ccccc12 |w:14.15|
Show InChI InChI=1S/C18H12N4O3/c23-18-14(12-5-1-3-7-15(12)20-18)9-11-10-19-21-17(11)13-6-2-4-8-16(13)22(24)25/h1-10H,(H,19,21)(H,20,23)
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n/an/a 1.20n/an/an/an/an/an/a



East China University of Science and Technology

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha (unknown origin) after 10 mins by mobility shift assay


Bioorg Med Chem 21: 1724-34 (2013)


Article DOI: 10.1016/j.bmc.2013.01.047
BindingDB Entry DOI: 10.7270/Q2GQ704N
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50192005
PNG
(CHEMBL3947262)
Show SMILES CN1CCN(CC1)c1ccccc1CNC(=O)c1ccc(F)c(NC(=O)c2cnn3cc(ccc23)-c2ccnn2C)c1
Show InChI InChI=1S/C31H31FN8O2/c1-37-13-15-39(16-14-37)28-6-4-3-5-22(28)18-33-30(41)21-7-9-25(32)26(17-21)36-31(42)24-19-35-40-20-23(8-10-29(24)40)27-11-12-34-38(27)2/h3-12,17,19-20H,13-16,18H2,1-2H3,(H,33,41)(H,36,42)
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n/an/a 1.20n/an/an/an/an/an/a



Novartis Institutes of Biomedical Research (NIBR)

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha kinase domain (unknown origin) assessed as reduction in probe peptide substrate phosphorylation by capillary electrophoresis


J Med Chem 59: 7901-14 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00703
BindingDB Entry DOI: 10.7270/Q25X2BW1
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50192006
PNG
(CHEMBL3955987)
Show SMILES Cn1nccc1-c1ccn2c(cnc2c1)C(=O)Nc1cc(ccc1F)C(=O)NCCN1CCCC1(C)C
Show InChI InChI=1S/C27H30FN7O2/c1-27(2)9-4-12-34(27)14-11-29-25(36)19-5-6-20(28)21(15-19)32-26(37)23-17-30-24-16-18(8-13-35(23)24)22-7-10-31-33(22)3/h5-8,10,13,15-17H,4,9,11-12,14H2,1-3H3,(H,29,36)(H,32,37)
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n/an/a 1.30n/an/an/an/an/an/a



Novartis Institutes of Biomedical Research (NIBR)

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha kinase domain (unknown origin) assessed as reduction in probe peptide substrate phosphorylation by capillary electrophoresis


J Med Chem 59: 7901-14 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00703
BindingDB Entry DOI: 10.7270/Q25X2BW1
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50345579
PNG
(5-((5-(4-((4-(2-hydroxyethyl)piperazin-1-yl)methyl...)
Show SMILES CNC(=O)c1ncc(C#Cc2cc(ccc2C)C(=O)Nc2ccc(CN3CCN(CCO)CC3)c(c2)C(F)(F)F)n1C
Show InChI InChI=1S/C30H33F3N6O3/c1-20-4-5-22(16-21(20)7-9-25-18-35-27(37(25)3)29(42)34-2)28(41)36-24-8-6-23(26(17-24)30(31,32)33)19-39-12-10-38(11-13-39)14-15-40/h4-6,8,16-18,40H,10-15,19H2,1-3H3,(H,34,42)(H,36,41)
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n/an/a 1.30n/an/an/an/an/an/a



ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL


Assay Description
Inhibition of human PDGFRalpha using poly[Glu:Tyr] by Hotspot assay


Bioorg Med Chem Lett 21: 3743-8 (2011)


Article DOI: 10.1016/j.bmcl.2011.04.060
BindingDB Entry DOI: 10.7270/Q21G0MM8
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50191972
PNG
(CHEMBL3895824)
Show SMILES C[C@H]1CCC[C@@H](C)N1CCNC(=O)c1ccc(F)c(NC(=O)c2cnc3cc(ccn23)-c2ccnn2C)c1 |r|
Show InChI InChI=1S/C28H32FN7O2/c1-18-5-4-6-19(2)35(18)14-12-30-27(37)21-7-8-22(29)23(15-21)33-28(38)25-17-31-26-16-20(10-13-36(25)26)24-9-11-32-34(24)3/h7-11,13,15-19H,4-6,12,14H2,1-3H3,(H,30,37)(H,33,38)/t18-,19+
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n/an/a 1.30n/an/an/an/an/an/a



Novartis Institutes of Biomedical Research (NIBR)

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha kinase domain (unknown origin) assessed as reduction in probe peptide substrate phosphorylation by capillary electrophoresis


J Med Chem 59: 7901-14 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00703
BindingDB Entry DOI: 10.7270/Q25X2BW1
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM106560
PNG
(US8586600, II-55)
Show SMILES CN(C)C\C=C\C(=O)Nc1ccc(cc1C(F)(F)F)C(=O)Nc1ccc(C)c(Nc2nccc(n2)-c2cccnc2)c1
Show InChI InChI=1S/C30H28F3N7O2/c1-19-8-10-22(17-26(19)39-29-35-14-12-24(38-29)21-6-4-13-34-18-21)36-28(42)20-9-11-25(23(16-20)30(31,32)33)37-27(41)7-5-15-40(2)3/h4-14,16-18H,15H2,1-3H3,(H,36,42)(H,37,41)(H,35,38,39)/b7-5+
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n/an/a 1.40n/an/an/an/an/an/a



Celgene Avilomics Research, Inc.

US Patent


Assay Description
Compounds may also be assayed as inhibitors of PDGFR in a manner substantially similar to the method described in Roberts, et al., “Antiangiogen...


US Patent US8586600 (2013)


BindingDB Entry DOI: 10.7270/Q2M61HWH
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50192007
PNG
(CHEMBL3902237)
Show SMILES CCN(CCNC(=O)c1ccc(F)c(NC(=O)c2cnc3cc(ccn23)-c2ccnn2C)c1)C(C)(C)C
Show InChI InChI=1S/C27H32FN7O2/c1-6-34(27(2,3)4)14-12-29-25(36)19-7-8-20(28)21(15-19)32-26(37)23-17-30-24-16-18(10-13-35(23)24)22-9-11-31-33(22)5/h7-11,13,15-17H,6,12,14H2,1-5H3,(H,29,36)(H,32,37)
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n/an/a 1.60n/an/an/an/an/an/a



Novartis Institutes of Biomedical Research (NIBR)

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha kinase domain (unknown origin) assessed as reduction in probe peptide substrate phosphorylation by capillary electrophoresis


J Med Chem 59: 7901-14 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00703
BindingDB Entry DOI: 10.7270/Q25X2BW1
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50162156
PNG
(1-(2,3-Difluoro-phenyl)-3-[4-(6,7-dimethoxy-quinol...)
Show SMILES COc1cc2nccc(Oc3ccc(NC(=O)Nc4cccc(F)c4F)cc3)c2cc1OC
Show InChI InChI=1S/C24H19F2N3O4/c1-31-21-12-16-19(13-22(21)32-2)27-11-10-20(16)33-15-8-6-14(7-9-15)28-24(30)29-18-5-3-4-17(25)23(18)26/h3-13H,1-2H3,(H2,28,29,30)
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n/an/a 1.60n/an/an/an/an/an/a



Kirin Brewery Co. Ltd.

Curated by ChEMBL


Assay Description
Inhibition of platelet-derived growth factor receptor alpha


J Med Chem 48: 1359-66 (2005)


Article DOI: 10.1021/jm030427r
BindingDB Entry DOI: 10.7270/Q23J3CG1
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50026612
PNG
(BIBF-1120 | Nintedanib | US10981896, Compound Nint...)
Show SMILES COC(=O)c1ccc2\C(=C(\Nc3ccc(cc3)N(C)C(=O)CN3CCN(C)CC3)c3ccccc3)C(=O)Nc2c1
Show InChI InChI=1S/C31H33N5O4/c1-34-15-17-36(18-16-34)20-27(37)35(2)24-12-10-23(11-13-24)32-29(21-7-5-4-6-8-21)28-25-14-9-22(31(39)40-3)19-26(25)33-30(28)38/h4-14,19,32H,15-18,20H2,1-3H3,(H,33,38)/b29-28-
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n/an/a 1.90n/an/an/an/an/an/a



Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University)

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha (unknown origin) preincubated for 10 mins followed by FAM-labeled peptide substrate addition measured after 1 hr by mobility...


Bioorg Med Chem 25: 1778-1786 (2017)


Article DOI: 10.1016/j.bmc.2017.01.039
BindingDB Entry DOI: 10.7270/Q20P127V
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM13530
PNG
(4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[...)
Show SMILES CN1CCN(Cc2ccc(cc2)C(=O)Nc2ccc(C)c(Nc3nccc(n3)-c3cccnc3)c2)CC1
Show InChI InChI=1S/C29H31N7O/c1-21-5-10-25(18-27(21)34-29-31-13-11-26(33-29)24-4-3-12-30-19-24)32-28(37)23-8-6-22(7-9-23)20-36-16-14-35(2)15-17-36/h3-13,18-19H,14-17,20H2,1-2H3,(H,32,37)(H,31,33,34)
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n/an/a 2n/an/an/an/an/an/a



Lilly Research Laboratories

Curated by ChEMBL


Assay Description
Inhibition of PDGFRA (unknown origin)


J Med Chem 56: 6991-7002 (2013)


Article DOI: 10.1021/jm400798j
BindingDB Entry DOI: 10.7270/Q2G44RQC
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50162152
PNG
(1-[4-(6,7-Dimethoxy-quinolin-4-yloxy)-phenyl]-3-(4...)
Show SMILES COc1ccc(NC(=O)Nc2ccc(Oc3ccnc4cc(OC)c(OC)cc34)cc2)cc1
Show InChI InChI=1S/C25H23N3O5/c1-30-18-8-4-16(5-9-18)27-25(29)28-17-6-10-19(11-7-17)33-22-12-13-26-21-15-24(32-3)23(31-2)14-20(21)22/h4-15H,1-3H3,(H2,27,28,29)
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n/an/a 2n/an/an/an/an/an/a



Kirin Brewery Co. Ltd.

Curated by ChEMBL


Assay Description
Inhibition of platelet-derived growth factor receptor alpha


J Med Chem 48: 1359-66 (2005)


Article DOI: 10.1021/jm030427r
BindingDB Entry DOI: 10.7270/Q23J3CG1
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50162145
PNG
(1-[4-(6,7-Dimethoxy-quinolin-4-yloxy)-phenyl]-3-(3...)
Show SMILES COc1cccc(NC(=O)Nc2ccc(Oc3ccnc4cc(OC)c(OC)cc34)cc2)c1
Show InChI InChI=1S/C25H23N3O5/c1-30-19-6-4-5-17(13-19)28-25(29)27-16-7-9-18(10-8-16)33-22-11-12-26-21-15-24(32-3)23(31-2)14-20(21)22/h4-15H,1-3H3,(H2,27,28,29)
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n/an/a 2n/an/an/an/an/an/a



Kirin Brewery Co. Ltd.

Curated by ChEMBL


Assay Description
Inhibition of platelet-derived growth factor receptor alpha


J Med Chem 48: 1359-66 (2005)


Article DOI: 10.1021/jm030427r
BindingDB Entry DOI: 10.7270/Q23J3CG1
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha/beta


(Homo sapiens (Human))
BDBM2579
PNG
((2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-2...)
Show SMILES CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r|
Show InChI InChI=1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1
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n/an/a 2n/an/an/an/an/an/a



Johnson & Johnson Pharmaceutical Research & Development

Curated by ChEMBL


Assay Description
Inhibition of Protein kinase C beta 1


Bioorg Med Chem Lett 13: 3049-53 (2003)


BindingDB Entry DOI: 10.7270/Q2DR2TVT
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50538442
PNG
(CHEMBL4638981)
Show SMILES Cc1ccc(cc1C#Cc1cnc2cccnn12)C(=O)Nc1ccc(CN2Cc3cn[nH]c3C2)c(Cl)c1
Show InChI InChI=1S/C28H22ClN7O/c1-18-4-5-20(11-19(18)7-9-24-14-30-27-3-2-10-32-36(24)27)28(37)33-23-8-6-21(25(29)12-23)15-35-16-22-13-31-34-26(22)17-35/h2-6,8,10-14H,15-17H2,1H3,(H,31,34)(H,33,37)
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n/an/a 2n/an/an/an/an/an/a



University of Oxford

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha (unknown origin) assessed as residual activity incubated for 5 mins in presence of [gamma-33ATP] by scintillation counting b...


ACS Med Chem Lett 11: 491-496 (2020)


Article DOI: 10.1021/acsmedchemlett.9b00612
BindingDB Entry DOI: 10.7270/Q2377D68
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50421033
PNG
(CHEMBL2087167)
Show SMILES CCN1CCC(CC1)Nc1ccc2NC(=O)C(=C(c3ncc(C)[nH]3)c3cccc(F)c3)c2c1 |w:17.25|
Show InChI InChI=1S/C26H28FN5O/c1-3-32-11-9-19(10-12-32)30-20-7-8-22-21(14-20)24(26(33)31-22)23(25-28-15-16(2)29-25)17-5-4-6-18(27)13-17/h4-8,13-15,19,30H,3,9-12H2,1-2H3,(H,28,29)(H,31,33)
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n/an/a 2n/an/an/an/an/an/a



Exelixis

Curated by ChEMBL


Assay Description
Inhibition of N-terminal GST-tagged PDGFRalpha after 2 hrs by luciferase-luciferin coupled chemiluminescence assay


Bioorg Med Chem Lett 22: 4979-85 (2012)


Article DOI: 10.1016/j.bmcl.2012.06.029
BindingDB Entry DOI: 10.7270/Q2XG9SD4
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50425780
PNG
(CHEMBL2316582)
Show SMILES CN1CCN(Cc2ccc(NC(=O)c3ccc(C)c(c3)C#Cc3cnc4[nH]ncc4c3)cc2C(F)(F)F)CC1
Show InChI InChI=1S/C29H27F3N6O/c1-19-3-5-22(14-21(19)6-4-20-13-24-17-34-36-27(24)33-16-20)28(39)35-25-8-7-23(26(15-25)29(30,31)32)18-38-11-9-37(2)10-12-38/h3,5,7-8,13-17H,9-12,18H2,1-2H3,(H,35,39)(H,33,34,36)
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n/an/a 2.10n/an/an/an/an/an/a


TBA



Citation and Details
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50538438
PNG
(CHEMBL4640297)
Show SMILES Cc1ccc(cc1C#Cc1cnc2cccnn12)C(=O)Nc1ccc(CN2CCC3C=NNC3C2)c(Cl)c1 |c:33|
Show InChI InChI=1S/C29H26ClN7O/c1-19-4-5-21(13-20(19)7-9-25-16-31-28-3-2-11-33-37(25)28)29(38)34-24-8-6-23(26(30)14-24)17-36-12-10-22-15-32-35-27(22)18-36/h2-6,8,11,13-16,22,27,35H,10,12,17-18H2,1H3,(H,34,38)
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n/an/a 2.10n/an/an/an/an/an/a



University of Oxford

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha (unknown origin) assessed as residual activity incubated for 5 mins in presence of [gamma-33ATP] by scintillation counting b...


ACS Med Chem Lett 11: 491-496 (2020)


Article DOI: 10.1021/acsmedchemlett.9b00612
BindingDB Entry DOI: 10.7270/Q2377D68
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM106553
PNG
(US8586600, II-2)
Show SMILES Cc1ccc(NC(=O)c2ccc(NC(=O)C=C)c(c2)C(F)(F)F)cc1Nc1nccc(n1)-c1cccnc1
Show InChI InChI=1S/C27H21F3N6O2/c1-3-24(37)34-22-9-7-17(13-20(22)27(28,29)30)25(38)33-19-8-6-16(2)23(14-19)36-26-32-12-10-21(35-26)18-5-4-11-31-15-18/h3-15H,1H2,2H3,(H,33,38)(H,34,37)(H,32,35,36)
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n/an/a 2.20n/an/an/an/an/an/a



Celgene Avilomics Research, Inc.

US Patent


Assay Description
Compounds may also be assayed as inhibitors of PDGFR in a manner substantially similar to the method described in Roberts, et al., “Antiangiogen...


US Patent US8586600 (2013)


BindingDB Entry DOI: 10.7270/Q2M61HWH
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50026612
PNG
(BIBF-1120 | Nintedanib | US10981896, Compound Nint...)
Show SMILES COC(=O)c1ccc2\C(=C(\Nc3ccc(cc3)N(C)C(=O)CN3CCN(C)CC3)c3ccccc3)C(=O)Nc2c1
Show InChI InChI=1S/C31H33N5O4/c1-34-15-17-36(18-16-34)20-27(37)35(2)24-12-10-23(11-13-24)32-29(21-7-5-4-6-8-21)28-25-14-9-22(31(39)40-3)19-26(25)33-30(28)38/h4-14,19,32H,15-18,20H2,1-3H3,(H,33,38)/b29-28-
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n/an/a 2.30n/an/an/an/an/an/a



Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University)

Curated by ChEMBL


Assay Description
Inhibition of N-terminal GST tagged human PDGFRalpha (550 to 1089 end residues) cytoplasmic domain expressed in baculovirus expression system preincu...


Eur J Med Chem 139: 492-502 (2017)


Article DOI: 10.1016/j.ejmech.2017.08.031
BindingDB Entry DOI: 10.7270/Q269762M
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50331095
PNG
(CHEMBL1289494 | Tivozanib | US10464902, Tivozanib)
Show SMILES COc1cc2nccc(Oc3ccc(NC(=O)Nc4cc(C)on4)c(Cl)c3)c2cc1OC
Show InChI InChI=1S/C22H19ClN4O5/c1-12-8-21(27-32-12)26-22(28)25-16-5-4-13(9-15(16)23)31-18-6-7-24-17-11-20(30-3)19(29-2)10-14(17)18/h4-11H,1-3H3,(H2,25,26,27,28)
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n/an/a 2.30n/an/an/an/an/an/a



Sichuan University

Curated by ChEMBL


Assay Description
Inhibition of recombinant PDGFRalpha (unknown origin) by cell-free assay


Bioorg Med Chem Lett 25: 2425-8 (2015)


Article DOI: 10.1016/j.bmcl.2015.03.088
BindingDB Entry DOI: 10.7270/Q2KW5HRT
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50604027
PNG
(CHEMBL5184634 | US20230312529, Compound 6i)
Show SMILES CCN1CCN(CC1)c1ccc(Nc2ncc(C)c(Nc3ccc4cn[nH]c4c3)n2)cc1OC
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n/an/a 2.40n/an/an/an/an/an/a


TBA



Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c01732
BindingDB Entry DOI: 10.7270/Q2QR527K
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50322535
PNG
(3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N...)
Show SMILES CN1CCN(Cc2ccc(NC(=O)c3ccc(C)c(c3)C#Cc3cnc4cccnn34)cc2C(F)(F)F)CC1
Show InChI InChI=1S/C29H27F3N6O/c1-20-5-6-22(16-21(20)8-10-25-18-33-27-4-3-11-34-38(25)27)28(39)35-24-9-7-23(26(17-24)29(30,31)32)19-37-14-12-36(2)13-15-37/h3-7,9,11,16-18H,12-15,19H2,1-2H3,(H,35,39)
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n/an/a 2.60n/an/an/an/an/an/a



Chinese Academy of Sciences

Curated by ChEMBL


Assay Description
Inhibition of recombinant PDGFRalpha (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA


Eur J Med Chem 126: 122-132 (2017)


Article DOI: 10.1016/j.ejmech.2016.10.003
BindingDB Entry DOI: 10.7270/Q2FX7CQK
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50604027
PNG
(CHEMBL5184634 | US20230312529, Compound 6i)
Show SMILES CCN1CCN(CC1)c1ccc(Nc2ncc(C)c(Nc3ccc4cn[nH]c4c3)n2)cc1OC
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n/an/a 2.70n/an/an/an/an/an/a


TBA



Citation and Details
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha


(Homo sapiens (Human))
BDBM50604027
PNG
(CHEMBL5184634 | US20230312529, Compound 6i)
Show SMILES CCN1CCN(CC1)c1ccc(Nc2ncc(C)c(Nc3ccc4cn[nH]c4c3)n2)cc1OC
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n/an/a 2.70n/an/an/an/an/an/a


TBA



Citation and Details
More data for this
Ligand-Target Pair
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