Reaction Details Report a problem with these data
Target
Platelet-derived growth factor receptor beta
Ligand
BDBM50191978
Substrate
n/a
Meas. Tech.
ChEMBL_1613238 (CHEMBL3855038)
IC50
13±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:
BDBM50191978
Synonyms:
CHEMBL3915941
Type:
Small organic molecule
Emp. Form.:
C27H32N8O2
Mol. Mass.:
500.5954
SMILES:
Cc1ncc(cc1NC(=O)c1cnn2cc(ccc12)-c1cnn(C)c1)C(=O)NCCN1CCCC1(C)C
Structure:
Search PDB for entries with ligand similarity: