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Compile Data Set for Download or QSAR

Found 651 hits Enz. Inhib. hit(s) with Target = 'Platelet-derived growth factor receptor'   
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


(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


J Med Chem 52: 3191-204 (2009)

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


(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


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

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


(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 0.600n/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)

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


(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


(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)

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


(Homo sapiens (Human))
BDBM50184769
PNG
(CHEMBL3823212)
Show SMILES CN(C)C1CCN(CCn2nc(-c3ccc(C)cc3)c3c(N)ncnc23)CC1
Show InChI InChI=1S/C21H29N7/c1-15-4-6-16(7-5-15)19-18-20(22)23-14-24-21(18)28(25-19)13-12-27-10-8-17(9-11-27)26(2)3/h4-7,14,17H,8-13H2,1-3H3,(H2,22,23,24)
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n/an/a>1n/an/an/an/an/an/a



University of Edinburgh

Curated by ChEMBL


Assay Description
Inhibition of human PDGFRalpha using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P]ATP


J Med Chem 59: 4697-710 (2016)

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


(Homo sapiens (Human))
BDBM50184770
PNG
(CHEMBL3823849)
Show SMILES CN(C)CC1CCN(CCn2nc(-c3ccc(C)cc3)c3c(N)ncnc23)CC1
Show InChI InChI=1S/C22H31N7/c1-16-4-6-18(7-5-16)20-19-21(23)24-15-25-22(19)29(26-20)13-12-28-10-8-17(9-11-28)14-27(2)3/h4-7,15,17H,8-14H2,1-3H3,(H2,23,24,25)
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University of Edinburgh

Curated by ChEMBL


Assay Description
Inhibition of human PDGFRalpha using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P]ATP


J Med Chem 59: 4697-710 (2016)

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


(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


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

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


(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)

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


(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)

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


(Homo sapiens (Human))
BDBM50184772
PNG
(CHEMBL3822591)
Show SMILES CN(C)CCC1CCN(CCn2nc(-c3ccc(C)cc3)c3c(N)ncnc23)CC1
Show InChI InChI=1S/C23H33N7/c1-17-4-6-19(7-5-17)21-20-22(24)25-16-26-23(20)30(27-21)15-14-29-12-9-18(10-13-29)8-11-28(2)3/h4-7,16,18H,8-15H2,1-3H3,(H2,24,25,26)
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University of Edinburgh

Curated by ChEMBL


Assay Description
Inhibition of human PDGFRalpha using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P]ATP


J Med Chem 59: 4697-710 (2016)

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


(Homo sapiens (Human))
BDBM50184774
PNG
(CHEMBL3799221)
Show SMILES CCOC(Cn1nc(-c2cnc3[nH]ccc3c2)c2c(N)ncnc12)OCC
Show InChI InChI=1S/C18H21N7O2/c1-3-26-13(27-4-2)9-25-18-14(16(19)22-10-23-18)15(24-25)12-7-11-5-6-20-17(11)21-8-12/h5-8,10,13H,3-4,9H2,1-2H3,(H,20,21)(H2,19,22,23)
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University of Edinburgh

Curated by ChEMBL


Assay Description
Inhibition of human PDGFRalpha using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P]ATP


J Med Chem 59: 4697-710 (2016)

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


(Homo sapiens (Human))
BDBM50184766
PNG
(CHEMBL3823861)
Show SMILES CN(C)CC1CCN(CCn2nc(-c3cnc4[nH]ccc4c3)c3c(N)ncnc23)CC1
Show InChI InChI=1S/C22H29N9/c1-29(2)13-15-4-7-30(8-5-15)9-10-31-22-18(20(23)26-14-27-22)19(28-31)17-11-16-3-6-24-21(16)25-12-17/h3,6,11-12,14-15H,4-5,7-10,13H2,1-2H3,(H,24,25)(H2,23,26,27)
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University of Edinburgh

Curated by ChEMBL


Assay Description
Inhibition of human PDGFRalpha using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P]ATP


J Med Chem 59: 4697-710 (2016)

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


(Homo sapiens (Human))
BDBM50184767
PNG
(CHEMBL3824089)
Show SMILES COc1cc(ccc1NC(=O)OC(C)(C)C)-c1nn(CCN2CCC(CC2)N(C)C)c2ncnc(N)c12
Show InChI InChI=1S/C26H38N8O3/c1-26(2,3)37-25(35)30-19-8-7-17(15-20(19)36-6)22-21-23(27)28-16-29-24(21)34(31-22)14-13-33-11-9-18(10-12-33)32(4)5/h7-8,15-16,18H,9-14H2,1-6H3,(H,30,35)(H2,27,28,29)
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University of Edinburgh

Curated by ChEMBL


Assay Description
Inhibition of human PDGFRalpha using poly[Glu,Tyr]4:1 as substrate in presence of [gamma-33P]ATP


J Med Chem 59: 4697-710 (2016)

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


(Mus musculus (mouse))
BDBM50446319
PNG
(CHEMBL3109343)
Show SMILES COCCOc1ccn2c(cnc2c1)-c1ccc2cccc(OCC3(F)CCNCC3)c2n1
Show InChI InChI=1S/C25H27FN4O3/c1-31-13-14-32-19-7-12-30-21(16-28-23(30)15-19)20-6-5-18-3-2-4-22(24(18)29-20)33-17-25(26)8-10-27-11-9-25/h2-7,12,15-16,27H,8-11,13-14,17H2,1H3
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n/an/a 1n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of PDGF-induced PDGFRbeta phosphorylation in mouse NIH3T3 cells incubated for 1 hr prior to PDGF induction measured after 15 mins by fluor...


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


(Mus musculus (mouse))
BDBM50446312
PNG
(CHEMBL3109350)
Show SMILES COCCOc1ccn2c(cnc2c1)-c1ccc2cccc(OCC3CCNC3)c2n1
Show InChI InChI=1S/C24H26N4O3/c1-29-11-12-30-19-8-10-28-21(15-26-23(28)13-19)20-6-5-18-3-2-4-22(24(18)27-20)31-16-17-7-9-25-14-17/h2-6,8,10,13,15,17,25H,7,9,11-12,14,16H2,1H3
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TBA

Assay Description
Inhibition of PDGF-induced PDGFRbeta phosphorylation in mouse NIH3T3 cells incubated for 1 hr prior to PDGF induction measured after 15 mins by fluor...


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


(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


Bioorg Med Chem 21: 1724-34 (2013)

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


(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)

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


(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


(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)

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


(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)

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


(Mus musculus (mouse))
BDBM50446315
PNG
(CHEMBL3109347)
Show SMILES COCCOc1ccn2c(cnc2c1)-c1ccc2cccc(O[C@@H]3CCNC[C@@H]3O)c2n1
Show InChI InChI=1S/C24H26N4O4/c1-30-11-12-31-17-8-10-28-19(14-26-23(28)13-17)18-6-5-16-3-2-4-22(24(16)27-18)32-21-7-9-25-15-20(21)29/h2-6,8,10,13-14,20-21,25,29H,7,9,11-12,15H2,1H3/t20-,21+/m0/s1
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n/an/a 2n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of PDGF-induced PDGFRbeta phosphorylation in mouse NIH3T3 cells incubated for 1 hr prior to PDGF induction measured after 15 mins by fluor...


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


(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)

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


(Mus musculus (mouse))
BDBM50384726
PNG
(CHEMBL2037208)
Show SMILES FC(F)(F)c1cccc(c1)C(=O)Nc1cccc(Nc2ccc3\C(=C\c4ccc[nH]4)C(=O)Nc3c2)c1
Show InChI InChI=1S/C27H19F3N4O2/c28-27(29,30)17-5-1-4-16(12-17)25(35)33-20-7-2-6-19(13-20)32-21-9-10-22-23(14-18-8-3-11-31-18)26(36)34-24(22)15-21/h1-15,31-32H,(H,33,35)(H,34,36)/b23-14-
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n/an/a 2n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of Tel-fused PDGFRbeta in mouse BA/F3 cells


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


(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


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

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


(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)

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


(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)

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


(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


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

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


(Mus musculus (mouse))
BDBM50446316
PNG
(CHEMBL3109346)
Show SMILES COCCOc1ccn2c(cnc2c1)-c1ccc2cccc(O[C@@H]3CCNC[C@H]3O)c2n1
Show InChI InChI=1S/C24H26N4O4/c1-30-11-12-31-17-8-10-28-19(14-26-23(28)13-17)18-6-5-16-3-2-4-22(24(16)27-18)32-21-7-9-25-15-20(21)29/h2-6,8,10,13-14,20-21,25,29H,7,9,11-12,15H2,1H3/t20-,21-/m1/s1
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TBA

Assay Description
Inhibition of PDGF-induced PDGFRbeta phosphorylation in mouse NIH3T3 cells incubated for 1 hr prior to PDGF induction measured after 15 mins by fluor...


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


(Mus musculus (mouse))
BDBM50446306
PNG
(CHEMBL3109340)
Show SMILES COCCOc1ccn2c(cnc2c1)-c1ccc2cccc(OC3CCNCC3)c2n1
Show InChI InChI=1S/C24H26N4O3/c1-29-13-14-30-19-9-12-28-21(16-26-23(28)15-19)20-6-5-17-3-2-4-22(24(17)27-20)31-18-7-10-25-11-8-18/h2-6,9,12,15-16,18,25H,7-8,10-11,13-14H2,1H3
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TBA

Assay Description
Inhibition of PDGF-induced PDGFRbeta phosphorylation in mouse NIH3T3 cells incubated for 1 hr prior to PDGF induction measured after 15 mins by fluor...


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


(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


J Med Chem 48: 1359-66 (2005)

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


(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


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

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


(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


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

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


(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


Bioorg Med Chem Lett 22: 3050-5 (2012)

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


(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


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

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


(Mus musculus (mouse))
BDBM50446304
PNG
(CHEMBL3109337)
Show SMILES COCCOc1ccn2c(cnc2c1)-c1ccc2cccc(O[C@@H]3CCNC[C@H]3F)c2n1
Show InChI InChI=1S/C24H25FN4O3/c1-30-11-12-31-17-8-10-29-20(15-27-23(29)13-17)19-6-5-16-3-2-4-22(24(16)28-19)32-21-7-9-26-14-18(21)25/h2-6,8,10,13,15,18,21,26H,7,9,11-12,14H2,1H3/t18-,21-/m1/s1
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TBA

Assay Description
Inhibition of PDGF-induced PDGFRbeta phosphorylation in mouse NIH3T3 cells incubated for 1 hr prior to PDGF induction measured after 15 mins by fluor...


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


(Mus musculus (mouse))
BDBM50446303
PNG
(CHEMBL3109338)
Show SMILES COCCOc1ccn2c(cnc2c1)-c1ccc2cccc(O[C@H]3CCNC[C@@H]3F)c2n1
Show InChI InChI=1S/C24H25FN4O3/c1-30-11-12-31-17-8-10-29-20(15-27-23(29)13-17)19-6-5-16-3-2-4-22(24(16)28-19)32-21-7-9-26-14-18(21)25/h2-6,8,10,13,15,18,21,26H,7,9,11-12,14H2,1H3/t18-,21-/m0/s1
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TBA

Assay Description
Inhibition of PDGF-induced PDGFRbeta phosphorylation in mouse NIH3T3 cells incubated for 1 hr prior to PDGF induction measured after 15 mins by fluor...


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


(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


J Med Chem 48: 1359-66 (2005)

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


(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


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

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


(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


J Med Chem 48: 1359-66 (2005)

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


(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


J Med Chem 48: 1359-66 (2005)

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


(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


J Med Chem 48: 1359-66 (2005)

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


(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


J Med Chem 48: 1359-66 (2005)

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


(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


J Med Chem 48: 1359-66 (2005)

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


(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


J Med Chem 48: 1359-66 (2005)

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


(Mus musculus (mouse))
BDBM50446305
PNG
(CHEMBL3109356)
Show SMILES COCCOc1ccn2c(cnc2c1)-c1ccc2cccc(O[C@@H]3CCNC[C@@H]3F)c2n1
Show InChI InChI=1S/C24H25FN4O3/c1-30-11-12-31-17-8-10-29-20(15-27-23(29)13-17)19-6-5-16-3-2-4-22(24(16)28-19)32-21-7-9-26-14-18(21)25/h2-6,8,10,13,15,18,21,26H,7,9,11-12,14H2,1H3/t18-,21+/m0/s1
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n/an/a 4n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of PDGF-induced PDGFRbeta phosphorylation in mouse NIH3T3 cells incubated for 1 hr prior to PDGF induction measured after 15 mins by fluor...


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


(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)


Bioorg Med Chem Lett 18: 5115-7 (2008)

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


(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


Eur J Med Chem 65: 477-86 (2013)

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


(Mus musculus (mouse))
BDBM50446304
PNG
(CHEMBL3109337)
Show SMILES COCCOc1ccn2c(cnc2c1)-c1ccc2cccc(O[C@@H]3CCNC[C@H]3F)c2n1
Show InChI InChI=1S/C24H25FN4O3/c1-30-11-12-31-17-8-10-29-20(15-27-23(29)13-17)19-6-5-16-3-2-4-22(24(16)28-19)32-21-7-9-26-14-18(21)25/h2-6,8,10,13,15,18,21,26H,7,9,11-12,14H2,1H3/t18-,21-/m1/s1
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n/an/a 4n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of PDGF-induced PDGFRbeta phosphorylation in mouse NIH3T3 cells incubated for 1 hr prior to PDGF induction measured after 15 mins by fluor...


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


(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


J Med Chem 49: 2186-92 (2006)

More data for this
Ligand-Target Pair
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