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Target
Platelet-derived growth factor receptor beta
Ligand
BDBM13530
Substrate
n/a
Meas. Tech.
ChEMBL_1613238 (CHEMBL3855038)
IC50
162±n/a nM
Citation
 Shaw, DE; Baig, F; Bruce, I; Chamoin, S; Collingwood, SP; Cross, S; Dayal, S; Drückes, P; Furet, P; Furminger, V; Haggart, D; Hussey, M; Konstantinova, I; Loren, JC; Molteni, V; Roberts, S; Reilly, J; Saunders, AM; Stringer, R; Sviridenko, L; Thomas, M; Thomson, CG; Tomlins, C; Wen, B; Yeh, V; Pearce, AC Optimization of Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for Duration of Action, as an Inhaled Therapy for Lung Remodeling in Pulmonary Arterial Hypertension. J Med Chem 59:7901-14 (2016) [PubMed]  Article 
Target
Name:
Platelet-derived growth factor receptor beta
Synonyms:
Beta-type platelet-derived growth factor receptor | CD140 antigen-like family member B | CD_antigen=CD140b | PDGF-R-beta | PGFRB_RAT | Pdgfr | Pdgfr1 | Pdgfrb | Platelet-derived growth factor receptor (PDGFr) | Platelet-derived growth factor receptor beta | Platelet-derived growth factor receptor beta (PDGFRB)
Type:
PROTEIN
Mol. Mass.:
122794.58
Organism:
Rattus norvegicus
Description:
ChEMBL_177425
Residue:
1097
Sequence:
MGLPEVMPASVLRGQLLLFVLLLLGPQISQGLVITPPGPEFVLNISSTFVLTCSSSAPVMWEQMSQVPWQEAAMNQDGTFSSVLTLTNVTGGDTGEYFCVYNNSLGPELSERKRIYIFVPDPTMGFLPMDSEDLFIFVTDVTETTIPCRVTDPQLEVTLHEKKVDIPLHVPYDHQRGFIGTFEDKTYICKTTIGDREVDSDTYYVYSLQVSSINVSVNAVQTVVRQGESITIRCIVMGNDVVNFQWTYPRMKSGRLVEPVTDYLFGVPSRIGSILHIPTAELSDSGTYTCNVSVSVNDHGDEKAINVTVIENGYVRLLETLEDVQIAELHRSRTLQVVFEAYPTPSVLWFKDNRTLGDSSAGELVLSTRNVSETRYVSELTLVRVKVSEAGYYTMRAFHADDQVQLSFKLQVNVPVRVLELSESHPANGEQILRCRGRGMPQPNVTWSTCRDLKRCPRKLSPTPLGNSSKEESQLETNVTFWEEDQEYEVVSTLRLRHVDQPLSVRCMLQNSMGRDSQEVTVVPHSLPFKVVVISAILALVVLTVISLIILIMLWQRKPRYEIRWKVIESVSSDGHEYIYVDPVQLPYDSTWELPRDQLVLGRTLGSGAFGQVVEATAHGLSHSQATMKVAVKMLKSTARSSEKQALMSELKIMSHLGPHLNVVNLLGACTKGGPIYIITEYCRYGDLVDYLHRNKHTFLQRHSNKHCPPSTELYSNALPVGLSLPSHLNLTGESDGGYMDMSKDESVDYVPMLDMKGHIKYADIESSSYMAPYDNYVPSAPERTYRATLINDSPVLSYTDLVGFSYQVANGMEFLASKNCVHRDLAARNVLICEGKLVKICDFGLARDIMRDSNYISKGSTFLPLKWMAPESIFNSLYTTLSDVWSFGILLWEIFTLGGTPYPELPMNDQFYNAIKRGYRMAQPAHASDEIYEIMQKCWEEKFETRPPFSQLVLLLERLLGEGYKKKYQQVDEEFLRSDHPAILRSQARLPGLHSLRSPLDTSSVLYTAVQPNETDNDYIIPLPDPKPDAADEGLLEGSPSLASSTLNEVNTSSTISCDSPLELQEEPQAEPEAQLEQPQDSGCPGPLAEAEDSFL
  
Inhibitor
Name:
BDBM13530
Synonyms:
4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide | CHEMBL941 | Gleevec | Imatinib | Imatinib, 21 | N-(4-methyl-3-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}phenyl)-4-[(4-methylpiperazin-1-yl)methyl]benzamide | STI-571 | STI571 | US10906896, Cpd imatinib | US11649218, Example Imatinib | US11725005, Compound imatinib | US9255107, Imatinib | cid_5291 | imatinib-CD3 | med.21724, Compound 6
Type:
Small organic molecule
Emp. Form.:
C29H31N7O
Mol. Mass.:
493.6027
SMILES:
CN1CCN(Cc2ccc(cc2)C(=O)Nc2ccc(C)c(Nc3nccc(n3)-c3cccnc3)c2)CC1
Structure:
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