Found 1098 hits of ic50 for UniProtKB: P16234 Target/Host (Institution) | Ligand | Target/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 | pH | Temp °C |
Platelet-derived growth factor receptor alpha
(Homo sapiens (Human)) | BDBM50191945
(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) | PDB
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UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 0.0900 | n/a | n/a | n/a | n/a | n/a | n/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
((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 | PDB
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Patents
Similars
| Article PubMed
| n/a | n/a | <0.100 | n/a | n/a | n/a | n/a | n/a | n/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
(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) | PDB
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UniProtKB/SwissProt
DrugBank antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | <0.100 | n/a | n/a | n/a | n/a | n/a | n/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
(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) | PDB
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| CHEMBL PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 0.180 | n/a | n/a | n/a | n/a | n/a | n/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
(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) | PDB
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| CHEMBL PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 0.190 | n/a | n/a | n/a | n/a | n/a | n/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
(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) | PDB
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DrugBank antibodypedia GoogleScholar AffyNet
| CHEMBL PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 0.200 | n/a | n/a | n/a | n/a | n/a | n/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
((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 | PDB
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| CHEMBL PC cid PC sid UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 0.240 | n/a | n/a | n/a | n/a | n/a | n/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
(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) | PDB
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| CHEMBL PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 0.320 | n/a | n/a | n/a | n/a | n/a | n/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
((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 | PDB
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Patents
Similars
| Article PubMed
| n/a | n/a | 0.418 | n/a | n/a | n/a | n/a | n/a | n/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
((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 | PDB
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CHEMBL MCE KEGG MMDB PC cid PC sid PDB UniChem
Patents
Similars
| Article PubMed
| n/a | n/a | 0.430 | n/a | n/a | n/a | n/a | n/a | n/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
((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 | PDB
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Patents
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| Article PubMed
| n/a | n/a | 0.450 | n/a | n/a | n/a | n/a | n/a | n/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
(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) | PDB
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| CHEMBL PC cid PC sid UniChem
Similars
| Article PubMed
| n/a | n/a | 0.530 | n/a | n/a | n/a | n/a | n/a | n/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
((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 | PDB
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Patents
Similars
| Article PubMed
| n/a | n/a | 0.580 | n/a | n/a | n/a | n/a | n/a | n/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
((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 | PDB
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Patents
Similars
| Article PubMed
| n/a | n/a | 0.600 | n/a | n/a | n/a | n/a | n/a | n/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
(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) | PDB
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Similars
| US Patent
| n/a | n/a | 0.730 | n/a | n/a | n/a | n/a | n/a | n/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
(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) | PDB
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| CHEMBL PC cid PC sid UniChem
| Article PubMed
| n/a | n/a | 0.75 | n/a | n/a | n/a | n/a | n/a | n/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
((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 | PDB
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Patents
Similars
| Article PubMed
| n/a | n/a | 0.793 | n/a | n/a | n/a | n/a | n/a | n/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
(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) | PDB
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| Article PubMed
| n/a | n/a | 0.960 | n/a | n/a | n/a | n/a | n/a | n/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
((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- | PDB
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| Article PubMed
| n/a | n/a | 0.980 | n/a | n/a | n/a | n/a | n/a | n/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
(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- | PDB
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| n/a | n/a | <1 | n/a | n/a | n/a | n/a | n/a | n/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
(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 | PDB
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| n/a | n/a | 1 | n/a | n/a | n/a | n/a | n/a | n/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
(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) | PDB
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| | n/a | n/a | 1 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
|
More data for this Ligand-Target Pair | |
Platelet-derived growth factor receptor alpha
(Homo sapiens (Human)) | BDBM50051957
(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- | PDB
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| n/a | n/a | <1 | n/a | n/a | n/a | n/a | n/a | n/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
(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) | PDB
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| n/a | n/a | 1.10 | n/a | n/a | n/a | n/a | n/a | n/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
(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) | PDB
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| n/a | n/a | 1.10 | n/a | n/a | n/a | n/a | n/a | n/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
(CHEMBL5176837)Show SMILES COc1cc2ncc(-c3cccc(NC4CCNC4)n3)n2cc1-c1cnn(C)c1 | PDB
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| n/a | n/a | 1.10 | n/a | n/a | n/a | n/a | n/a | n/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
(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) | PDB
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| n/a | n/a | 1.20 | n/a | n/a | n/a | n/a | n/a | n/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
(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) | PDB
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| n/a | n/a | 1.20 | n/a | n/a | n/a | n/a | n/a | n/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
(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) | PDB
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| n/a | n/a | 1.30 | n/a | n/a | n/a | n/a | n/a | n/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
(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) | PDB
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| n/a | n/a | 1.30 | n/a | n/a | n/a | n/a | n/a | n/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
(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+ | PDB
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| n/a | n/a | 1.30 | n/a | n/a | n/a | n/a | n/a | n/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
(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+ | PDB
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| US Patent
| n/a | n/a | 1.40 | n/a | n/a | n/a | n/a | n/a | n/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
(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) | PDB
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| n/a | n/a | 1.60 | n/a | n/a | n/a | n/a | n/a | n/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
(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) | PDB
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| n/a | n/a | 1.60 | n/a | n/a | n/a | n/a | n/a | n/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
(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- | PDB
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| n/a | n/a | 1.90 | n/a | n/a | n/a | n/a | n/a | n/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
(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) | PDB
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| n/a | n/a | 2 | n/a | n/a | n/a | n/a | n/a | n/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
(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) | PDB
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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
(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) | PDB
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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
((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 | PDB
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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
(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) | PDB
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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
(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) | PDB
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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
(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) | PDB
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| | n/a | n/a | 2.10 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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More data for this Ligand-Target Pair | |
Platelet-derived growth factor receptor alpha
(Homo sapiens (Human)) | BDBM50538438
(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) | PDB
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| n/a | n/a | 2.10 | n/a | n/a | n/a | n/a | n/a | n/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
(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) | PDB
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| n/a | n/a | 2.20 | n/a | n/a | n/a | n/a | n/a | n/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
(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- | PDB
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| n/a | n/a | 2.30 | n/a | n/a | n/a | n/a | n/a | n/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
(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) | PDB
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| n/a | n/a | 2.30 | n/a | n/a | n/a | n/a | n/a | n/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
(CHEMBL5184634 | US20230312529, Compound 6i)Show SMILES CCN1CCN(CC1)c1ccc(Nc2ncc(C)c(Nc3ccc4cn[nH]c4c3)n2)cc1OC | PDB
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TBA
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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
(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) | PDB
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| n/a | n/a | 2.60 | n/a | n/a | n/a | n/a | n/a | n/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
(CHEMBL5184634 | US20230312529, Compound 6i)Show SMILES CCN1CCN(CC1)c1ccc(Nc2ncc(C)c(Nc3ccc4cn[nH]c4c3)n2)cc1OC | PDB
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| | n/a | n/a | 2.70 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
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More data for this Ligand-Target Pair | |
Platelet-derived growth factor receptor alpha
(Homo sapiens (Human)) | BDBM50604027
(CHEMBL5184634 | US20230312529, Compound 6i)Show SMILES CCN1CCN(CC1)c1ccc(Nc2ncc(C)c(Nc3ccc4cn[nH]c4c3)n2)cc1OC | PDB
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| | n/a | n/a | 2.70 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
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Citation and Details
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More data for this Ligand-Target Pair | |