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Target
Platelet-derived growth factor receptor beta
Ligand
BDBM50191973
Substrate
n/a
Meas. Tech.
ChEMBL_1613238 (CHEMBL3855038)
IC50
1.7±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:
BDBM50191973
Synonyms:
CHEMBL3940697
Type:
Small organic molecule
Emp. Form.:
C27H30FN7O2
Mol. Mass.:
503.5712
SMILES:
Cn1cc(cn1)-c1ccn2c(cnc2c1)C(=O)Nc1cc(ccc1F)C(=O)NCCN1CCCC1(C)C
Structure:
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