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Found 470 hits Enz. Inhib. hit(s) with Target = 'Platelet-derived growth factor receptor alpha (PDGFR alpha)' AND taxid = 9606   
Target
(Institution)
LigandTarget
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
Platelet-derived growth factor receptor alpha (PDGFR alpha)


(Homo sapiens (Human))
BDBM50381716
PNG
(ABT-348 | ILORASERTIB | US8722890, 1 | US8722890, ...)
Show SMILES Nc1ncc(-c2cnn(CCO)c2)c2scc(-c3ccc(NC(=O)Nc4cccc(F)c4)cc3)c12
Show InChI InChI=1S/C25H21FN6O2S/c26-17-2-1-3-19(10-17)31-25(34)30-18-6-4-15(5-7-18)21-14-35-23-20(12-28-24(27)22(21)23)16-11-29-32(13-16)8-9-33/h1-7,10-14,33H,8-9H2,(H2,27,28)(H2,30,31,34)
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0.794n/an/an/an/an/an/an/an/a


TBA

Assay Description
Inhibition of PDGFRA


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


(Homo sapiens (Human))
BDBM50388873
PNG
(CHEMBL1964441)
Show SMILES CNCC#Cc1cnc(N)c2c(csc12)-c1ccc(NC(=O)Nc2cccc(C)c2)cc1
Show InChI InChI=1S/C25H23N5OS/c1-16-5-3-7-20(13-16)30-25(31)29-19-10-8-17(9-11-19)21-15-32-23-18(6-4-12-27-2)14-28-24(26)22(21)23/h3,5,7-11,13-15,27H,12H2,1-2H3,(H2,26,28)(H2,29,30,31)
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Article
2.5n/an/an/an/an/an/an/an/a


TBA

Assay Description
Inhibition of PDGFRA


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


(Homo sapiens (Human))
BDBM50381703
PNG
(CHEMBL1970317)
Show SMILES Cn1cc(cn1)-c1cnc(N)c2c(csc12)-c1ccc(NC(=O)Nc2cccc(F)c2)cc1
Show InChI InChI=1S/C24H19FN6OS/c1-31-12-15(10-28-31)19-11-27-23(26)21-20(13-33-22(19)21)14-5-7-17(8-6-14)29-24(32)30-18-4-2-3-16(25)9-18/h2-13H,1H3,(H2,26,27)(H2,29,30,32)
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50n/an/an/an/an/an/an/an/a


TBA

Assay Description
Inhibition of PDGFRA


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


(Homo sapiens (Human))
BDBM50341519
PNG
((S)-3-(4-(2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl...)
Show SMILES CNc1cncc(n1)-c1c[nH]c(=O)c(NC(=O)c2ccc(cc2)N2CCC[C@H]2CN2CCCC2)c1
Show InChI InChI=1S/C26H31N7O2/c1-27-24-16-28-15-23(30-24)19-13-22(26(35)29-14-19)31-25(34)18-6-8-20(9-7-18)33-12-4-5-21(33)17-32-10-2-3-11-32/h6-9,13-16,21H,2-5,10-12,17H2,1H3,(H,27,30)(H,29,35)(H,31,34)/t21-/m0/s1
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>1.00E+3n/an/an/an/an/an/an/an/a



Vertex Pharmaceuticals (Europe) Ltd.

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha


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


(Homo sapiens (Human))
BDBM50388880
PNG
(CHEMBL1979577)
Show SMILES Cc1cccc(NC(=O)Nc2ccc(cc2)-c2csc3c(cnc(N)c23)C#CC(C)(C)N)c1
Show InChI InChI=1S/C26H25N5OS/c1-16-5-4-6-20(13-16)31-25(32)30-19-9-7-17(8-10-19)21-15-33-23-18(11-12-26(2,3)28)14-29-24(27)22(21)23/h4-10,13-15H,28H2,1-3H3,(H2,27,29)(H2,30,31,32)
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<1.00E+4n/an/an/an/an/an/an/an/a


TBA

Assay Description
Inhibition of PDGFRA


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


(Homo sapiens (Human))
BDBM50388874
PNG
(CHEMBL1967720)
Show SMILES CC(C)(C(N)=O)n1cc(cn1)-c1cnc(N)c2c(csc12)-c1ccc(NC(=O)Nc2cccc(F)c2)cc1
Show InChI InChI=1S/C27H24FN7O2S/c1-27(2,25(30)36)35-13-16(11-32-35)20-12-31-24(29)22-21(14-38-23(20)22)15-6-8-18(9-7-15)33-26(37)34-19-5-3-4-17(28)10-19/h3-14H,1-2H3,(H2,29,31)(H2,30,36)(H2,33,34,37)
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<1.00E+4n/an/an/an/an/an/an/an/a


TBA

Assay Description
Inhibition of PDGFRA


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


(Homo sapiens (Human))
BDBM50381719
PNG
(CHEMBL2022856)
Show SMILES C[C@@H](O)Cn1cc(cn1)-c1cnc(N)c2c(csc12)-c1ccc(NC(=O)Nc2cccc(F)c2)cc1
Show InChI InChI=1S/C26H23FN6O2S/c1-15(34)12-33-13-17(10-30-33)21-11-29-25(28)23-22(14-36-24(21)23)16-5-7-19(8-6-16)31-26(35)32-20-4-2-3-18(27)9-20/h2-11,13-15,34H,12H2,1H3,(H2,28,29)(H2,31,32,35)/t15-/m1/s1
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<1.00E+4n/an/an/an/an/an/an/an/a


TBA

Assay Description
Inhibition of PDGFRA


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


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


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

More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha (PDGFR 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


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


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


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


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


(Homo sapiens (Human))
BDBM50431812
PNG
(CHEMBL2347053)
Show SMILES [O-][N+](=O)c1ccccc1-c1n[nH]cc1C=C1C(=O)Nc2ccccc12
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


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


Citation and Details
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha (PDGFR 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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US Patent
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)

More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha (PDGFR 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


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


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


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


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


(Homo sapiens (Human))
BDBM50421033
PNG
(CHEMBL2087167)
Show SMILES CCN1CCC(CC1)Nc1ccc2NC(=O)C(=C(c3ncc(C)[nH]3)c3cccc(F)c3)c2c1
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


Citation and Details
More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha (PDGFR 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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US Patent
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)

More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha (PDGFR alpha)


(Homo sapiens (Human))
BDBM50331095
PNG
(CHEMBL1289494 | 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


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


(Homo sapiens (Human))
BDBM50381926
PNG
(CHEMBL2023489 | CHEMBL2023803)
Show SMILES COc1ccc2c(Oc3ccc(CC(=O)Nc4cn(C)nc4C)c(OC)c3)ccnc2c1
Show InChI InChI=1S/C24H24N4O4/c1-15-21(14-28(2)27-15)26-24(29)11-16-5-6-18(13-23(16)31-4)32-22-9-10-25-20-12-17(30-3)7-8-19(20)22/h5-10,12-14H,11H2,1-4H3,(H,26,29)
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n/an/a 3n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha


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


(Homo sapiens (Human))
BDBM50421026
PNG
(CHEMBL2086753)
Show SMILES CCN1CCC(CC1)Nc1ccc2NC(=O)C(=C(c3nc4ccccc4[nH]3)c3ccccc3)c2c1
Show InChI InChI=1S/C29H29N5O/c1-2-34-16-14-20(15-17-34)30-21-12-13-23-22(18-21)27(29(35)33-23)26(19-8-4-3-5-9-19)28-31-24-10-6-7-11-25(24)32-28/h3-13,18,20,30H,2,14-17H2,1H3,(H,31,32)(H,33,35)
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n/an/a 3n/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


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


(Homo sapiens (Human))
BDBM50420996
PNG
(CHEMBL2086760)
Show SMILES CCN1CCC(CC1)Nc1ccc2NC(=O)C(=C(c3ncc[nH]3)c3ccc(Cl)cc3)c2c1
Show InChI InChI=1S/C25H26ClN5O/c1-2-31-13-9-18(10-14-31)29-19-7-8-21-20(15-19)23(25(32)30-21)22(24-27-11-12-28-24)16-3-5-17(26)6-4-16/h3-8,11-12,15,18,29H,2,9-10,13-14H2,1H3,(H,27,28)(H,30,32)
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n/an/a 3n/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


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


(Homo sapiens (Human))
BDBM50162166
PNG
(1-[2-Chloro-4-(6,7-dimethoxy-quinolin-4-yloxy)-phe...)
Show SMILES COc1cc2nccc(Oc3ccc(NC(=O)Nc4ccc(F)cc4F)c(Cl)c3)c2cc1OC
Show InChI InChI=1S/C24H18ClF2N3O4/c1-32-22-11-15-20(12-23(22)33-2)28-8-7-21(15)34-14-4-6-18(16(25)10-14)29-24(31)30-19-5-3-13(26)9-17(19)27/h3-12H,1-2H3,(H2,29,30,31)
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n/an/a<3n/an/an/an/an/an/a



Kirin Brewery Co. Ltd.

Curated by ChEMBL


Assay Description
Inhibition of platelet-derived growth factor receptor alpha in cell-intact assay


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


(Homo sapiens (Human))
BDBM50421034
PNG
(CHEMBL2087168)
Show SMILES CCN1CCC(CC1)Nc1ccc2NC(=O)C(=C(c3ncc(C)[nH]3)c3cc(F)cc(F)c3)c2c1
Show InChI InChI=1S/C26H27F2N5O/c1-3-33-8-6-19(7-9-33)31-20-4-5-22-21(13-20)24(26(34)32-22)23(25-29-14-15(2)30-25)16-10-17(27)12-18(28)11-16/h4-5,10-14,19,31H,3,6-9H2,1-2H3,(H,29,30)(H,32,34)
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n/an/a 3n/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


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


(Homo sapiens (Human))
BDBM50162143
PNG
(1-[4-(6,7-Dimethoxy-quinolin-4-yloxy)-phenyl]-3-m-...)
Show SMILES COc1cc2nccc(Oc3ccc(NC(=O)Nc4cccc(C)c4)cc3)c2cc1OC
Show InChI InChI=1S/C25H23N3O4/c1-16-5-4-6-18(13-16)28-25(29)27-17-7-9-19(10-8-17)32-22-11-12-26-21-15-24(31-3)23(30-2)14-20(21)22/h4-15H,1-3H3,(H2,27,28,29)
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n/an/a 3.30n/an/an/an/an/an/a



Kirin Brewery Co. Ltd.

Curated by ChEMBL


Assay Description
Inhibition of platelet-derived growth factor receptor alpha


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


(Homo sapiens (Human))
BDBM50331095
PNG
(CHEMBL1289494 | 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 3.30n/an/an/an/an/an/a



Sichuan University

Curated by ChEMBL


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


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


(Homo sapiens (Human))
BDBM50162148
PNG
(1-(2,4-Difluoro-phenyl)-3-[4-(6,7-dimethoxy-quinol...)
Show SMILES COc1cc2nccc(Oc3ccc(NC(=O)Nc4ccc(F)cc4F)cc3)c2cc1OC
Show InChI InChI=1S/C24H19F2N3O4/c1-31-22-12-17-20(13-23(22)32-2)27-10-9-21(17)33-16-6-4-15(5-7-16)28-24(30)29-19-8-3-14(25)11-18(19)26/h3-13H,1-2H3,(H2,28,29,30)
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n/an/a 3.40n/an/an/an/an/an/a



Kirin Brewery Co. Ltd.

Curated by ChEMBL


Assay Description
Inhibition of platelet-derived growth factor receptor alpha


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


(Homo sapiens (Human))
BDBM50162170
PNG
(1-(2,6-Difluoro-phenyl)-3-[4-(6,7-dimethoxy-quinol...)
Show SMILES COc1cc2nccc(Oc3ccc(NC(=O)Nc4c(F)cccc4F)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)29-23-17(25)4-3-5-18(23)26/h3-13H,1-2H3,(H2,28,29,30)
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n/an/a 3.5n/an/an/an/an/an/a



Kirin Brewery Co. Ltd.

Curated by ChEMBL


Assay Description
Inhibition of platelet-derived growth factor receptor alpha


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


(Homo sapiens (Human))
BDBM50162157
PNG
(1-[4-(6,7-Dimethoxy-quinazolin-4-yloxy)-phenyl]-3-...)
Show SMILES COc1ccc(NC(=O)Nc2ccc(Oc3ncnc4cc(OC)c(OC)cc34)cc2)cc1
Show InChI InChI=1S/C24H22N4O5/c1-30-17-8-4-15(5-9-17)27-24(29)28-16-6-10-18(11-7-16)33-23-19-12-21(31-2)22(32-3)13-20(19)25-14-26-23/h4-14H,1-3H3,(H2,27,28,29)
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n/an/a 3.60n/an/an/an/an/an/a



Kirin Brewery Co. Ltd.

Curated by ChEMBL


Assay Description
Inhibition of platelet-derived growth factor receptor alpha


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


(Homo sapiens (Human))
BDBM50162150
PNG
(1-[4-(6,7-Dimethoxy-quinolin-4-yloxy)-phenyl]-3-o-...)
Show SMILES COc1cc2nccc(Oc3ccc(NC(=O)Nc4ccccc4C)cc3)c2cc1OC
Show InChI InChI=1S/C25H23N3O4/c1-16-6-4-5-7-20(16)28-25(29)27-17-8-10-18(11-9-17)32-22-12-13-26-21-15-24(31-3)23(30-2)14-19(21)22/h4-15H,1-3H3,(H2,27,28,29)
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n/an/a 3.60n/an/an/an/an/an/a



Kirin Brewery Co. Ltd.

Curated by ChEMBL


Assay Description
Inhibition of platelet-derived growth factor receptor alpha


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


(Homo sapiens (Human))
BDBM50162167
PNG
(1-[4-(6,7-Dimethoxy-quinolin-4-yloxy)-phenyl]-3-ph...)
Show SMILES COc1cc2nccc(Oc3ccc(NC(=O)Nc4ccccc4)cc3)c2cc1OC
Show InChI InChI=1S/C24H21N3O4/c1-29-22-14-19-20(15-23(22)30-2)25-13-12-21(19)31-18-10-8-17(9-11-18)27-24(28)26-16-6-4-3-5-7-16/h3-15H,1-2H3,(H2,26,27,28)
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n/an/a 3.60n/an/an/an/an/an/a



Kirin Brewery Co. Ltd.

Curated by ChEMBL


Assay Description
Inhibition of platelet-derived growth factor receptor alpha


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


(Homo sapiens (Human))
BDBM50162142
PNG
(1-[4-(6,7-Dimethoxy-quinolin-4-yloxy)-phenyl]-3-(2...)
Show SMILES COc1cc2nccc(Oc3ccc(NC(=O)Nc4ccccc4F)cc3)c2cc1OC
Show InChI InChI=1S/C24H20FN3O4/c1-30-22-13-17-20(14-23(22)31-2)26-12-11-21(17)32-16-9-7-15(8-10-16)27-24(29)28-19-6-4-3-5-18(19)25/h3-14H,1-2H3,(H2,27,28,29)
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n/an/a 3.90n/an/an/an/an/an/a



Kirin Brewery Co. Ltd.

Curated by ChEMBL


Assay Description
Inhibition of platelet-derived growth factor receptor alpha


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


(Homo sapiens (Human))
BDBM50184857
PNG
(CHEMBL203227 | N-{4-[(6,7-Dimethoxy-4-quinolyl)oxy...)
Show SMILES COc1cc2nccc(Oc3ccc(NC(=O)NC(=O)c4ccccc4C)cc3)c2cc1OC
Show InChI InChI=1S/C26H23N3O5/c1-16-6-4-5-7-19(16)25(30)29-26(31)28-17-8-10-18(11-9-17)34-22-12-13-27-21-15-24(33-3)23(32-2)14-20(21)22/h4-15H,1-3H3,(H2,28,29,30,31)
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n/an/a 4n/an/an/an/an/an/a



Kirin Brewery Co., Ltd.

Curated by ChEMBL


Assay Description
Inhibition of PDGFR alpha phosphorylation in G292 cell


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


(Homo sapiens (Human))
BDBM50264389
PNG
(6-chloro-N-(pyrimidin-5-yl)-3-(3-(trifluoromethyl)...)
Show SMILES FC(F)(F)c1cccc(Nc2noc3c(C(=O)Nc4cncnc4)c(Cl)ccc23)c1
Show InChI InChI=1S/C19H11ClF3N5O2/c20-14-5-4-13-16(15(14)18(29)27-12-7-24-9-25-8-12)30-28-17(13)26-11-3-1-2-10(6-11)19(21,22)23/h1-9H,(H,26,28)(H,27,29)
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n/an/a 4n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha (unknown origin)


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


(Homo sapiens (Human))
BDBM50279080
PNG
((Z)-3-[(4-{Methyl-[2-(4-methylpiperazin-1-yl)acety...)
Show SMILES COC(=O)c1ccc2C(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/h4-14,19,28H,15-18,20H2,1-3H3,(H,33,38)
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n/an/a 4n/an/an/an/an/an/a



East China University of Science and Technology

Curated by ChEMBL


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


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


(Homo sapiens (Human))
BDBM50399537
PNG
(CHEMBL2180604)
Show SMILES Cc1cc(C(=O)Nc2cc(Oc3ccc4nc(NC(=O)C5CC5)cn4n3)ccc2C)n(C)n1
Show InChI InChI=1S/C23H23N7O3/c1-13-4-7-16(11-17(13)24-23(32)18-10-14(2)27-29(18)3)33-21-9-8-20-25-19(12-30(20)28-21)26-22(31)15-5-6-15/h4,7-12,15H,5-6H2,1-3H3,(H,24,32)(H,26,31)
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n/an/a 4.30n/an/an/an/an/an/a



Takeda Pharmaceutical Company Limited

Curated by ChEMBL


Assay Description
Inhibition of PDGFRalpha (unknown origin) by AlphaScreen assay


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


(Homo sapiens (Human))
BDBM50162169
PNG
(1-(2,5-Difluoro-phenyl)-3-[4-(6,7-dimethoxy-quinol...)
Show SMILES COc1cc2nccc(Oc3ccc(NC(=O)Nc4cc(F)ccc4F)cc3)c2cc1OC
Show InChI InChI=1S/C24H19F2N3O4/c1-31-22-12-17-19(13-23(22)32-2)27-10-9-21(17)33-16-6-4-15(5-7-16)28-24(30)29-20-11-14(25)3-8-18(20)26/h3-13H,1-2H3,(H2,28,29,30)
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n/an/a 4.70n/an/an/an/an/an/a



Kirin Brewery Co. Ltd.

Curated by ChEMBL


Assay Description
Inhibition of platelet-derived growth factor receptor alpha


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


(Homo sapiens (Human))
BDBM50184863
PNG
(CHEMBL202919 | N-(2-Chlorobenzoyl)-N'-{4-[(6,7-dim...)
Show SMILES COc1cc2nccc(Oc3ccc(NC(=S)NC(=O)c4ccccc4Cl)cc3)c2cc1OC
Show InChI InChI=1S/C25H20ClN3O4S/c1-31-22-13-18-20(14-23(22)32-2)27-12-11-21(18)33-16-9-7-15(8-10-16)28-25(34)29-24(30)17-5-3-4-6-19(17)26/h3-14H,1-2H3,(H2,28,29,30,34)
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n/an/a 5n/an/an/an/an/an/a



Kirin Brewery Co., Ltd.

Curated by ChEMBL


Assay Description
Inhibition of PDGFR alpha phosphorylation in G292 cell


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


(Homo sapiens (Human))
BDBM50421032
PNG
(CHEMBL2086754)
Show SMILES CCN1CCC(CC1)Nc1ccc2NC(=O)C(=C(c3nc4ccccc4[nH]3)c3ccc(C)cc3)c2c1
Show InChI InChI=1S/C30H31N5O/c1-3-35-16-14-21(15-17-35)31-22-12-13-24-23(18-22)28(30(36)34-24)27(20-10-8-19(2)9-11-20)29-32-25-6-4-5-7-26(25)33-29/h4-13,18,21,31H,3,14-17H2,1-2H3,(H,32,33)(H,34,36)
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n/an/a 5n/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


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


(Homo sapiens (Human))
BDBM50421035
PNG
(CHEMBL2087169)
Show SMILES CCN1CCC(CC1)Nc1ccc2NC(=O)C(=C(c3ncc(C)[nH]3)c3ccccc3F)c2c1
Show InChI InChI=1S/C26H28FN5O/c1-3-32-12-10-17(11-13-32)30-18-8-9-22-20(14-18)24(26(33)31-22)23(25-28-15-16(2)29-25)19-6-4-5-7-21(19)27/h4-9,14-15,17,30H,3,10-13H2,1-2H3,(H,28,29)(H,31,33)
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n/an/a 5n/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


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


(Homo sapiens (Human))
BDBM50184860
PNG
(CHEMBL380703 | Phenyl N-{4-[(6,7-Dimethoxy-4-quino...)
Show SMILES COc1cc2nccc(Oc3ccc(NC(=O)Oc4ccccc4)cc3)c2cc1OC
Show InChI InChI=1S/C24H20N2O5/c1-28-22-14-19-20(15-23(22)29-2)25-13-12-21(19)30-18-10-8-16(9-11-18)26-24(27)31-17-6-4-3-5-7-17/h3-15H,1-2H3,(H,26,27)
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n/an/a 5n/an/an/an/an/an/a



Kirin Brewery Co., Ltd.

Curated by ChEMBL


Assay Description
Inhibition of PDGFR alpha phosphorylation in G292 cell


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


(Homo sapiens (Human))
BDBM50162154
PNG
(1-[4-(6,7-Dimethoxy-quinolin-4-yloxy)-phenyl]-3-(2...)
Show SMILES COc1ccccc1NC(=O)Nc1ccc(Oc2ccnc3cc(OC)c(OC)cc23)cc1
Show InChI InChI=1S/C25H23N3O5/c1-30-22-7-5-4-6-19(22)28-25(29)27-16-8-10-17(11-9-16)33-21-12-13-26-20-15-24(32-3)23(31-2)14-18(20)21/h4-15H,1-3H3,(H2,27,28,29)
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n/an/a 5.80n/an/an/an/an/an/a



Kirin Brewery Co. Ltd.

Curated by ChEMBL


Assay Description
Inhibition of platelet-derived growth factor receptor alpha


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


(Homo sapiens (Human))
BDBM50162168
PNG
(1-[4-(6,7-Dimethoxy-quinolin-4-yloxy)-phenyl]-3-(4...)
Show SMILES COc1cc2nccc(Oc3ccc(NC(=O)Nc4ccc(F)cc4)cc3)c2cc1OC
Show InChI InChI=1S/C24H20FN3O4/c1-30-22-13-19-20(14-23(22)31-2)26-12-11-21(19)32-18-9-7-17(8-10-18)28-24(29)27-16-5-3-15(25)4-6-16/h3-14H,1-2H3,(H2,27,28,29)
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n/an/a 5.80n/an/an/an/an/an/a



Kirin Brewery Co. Ltd.

Curated by ChEMBL


Assay Description
Inhibition of platelet-derived growth factor receptor alpha


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


(Homo sapiens (Human))
BDBM106561
PNG
(US8586600, III-6)
Show SMILES CN(C)C\C=C\C(=O)Nc1ccc(NC(=O)c2ccc(C)c(Nc3nccc(n3)-c3cccnc3)c2)cc1C(F)(F)F
Show InChI InChI=1S/C30H28F3N7O2/c1-19-8-9-20(16-26(19)39-29-35-14-12-24(38-29)21-6-4-13-34-18-21)28(42)36-22-10-11-25(23(17-22)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 5.90n/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)

More data for this
Ligand-Target Pair
Platelet-derived growth factor receptor alpha (PDGFR alpha)


(Homo sapiens (Human))
BDBM50421031
PNG
(CHEMBL2086759)
Show SMILES CCN1CCC(CC1)Nc1ccc2NC(=O)C(=C(c3ncc[nH]3)c3cccc(F)c3)c2c1
Show InChI InChI=1S/C25H26FN5O/c1-2-31-12-8-18(9-13-31)29-19-6-7-21-20(15-19)23(25(32)30-21)22(24-27-10-11-28-24)16-4-3-5-17(26)14-16/h3-7,10-11,14-15,18,29H,2,8-9,12-13H2,1H3,(H,27,28)(H,30,32)
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n/an/a 6n/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


Citation and Details
More data for this
Ligand-Target Pair
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