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Target
TGF-beta receptor type-2
Ligand
BDBM50468191
Substrate
n/a
Meas. Tech.
ChEMBL_1798298 (CHEMBL4270415)
IC50
40±n/a nM
Citation
 Zhang, Y; Zhao, Y; Tebben, AJ; Sheriff, S; Ruzanov, M; Fereshteh, MP; Fan, Y; Lippy, J; Swanson, J; Ho, CP; Wautlet, BS; Rose, A; Parrish, K; Yang, Z; Donnell, AF; Zhang, L; Fink, BE; Vite, GD; Augustine-Rauch, K; Fargnoli, J; Borzilleri, RM Discovery of 4-Azaindole Inhibitors of TGF?RI as Immuno-oncology Agents. ACS Med Chem Lett 9:1117-1122 (2018) [PubMed]  Article 
Target
Name:
TGF-beta receptor type-2
Synonyms:
TGF-beta receptor type II | TGFBR2 | TGFR2_HUMAN
Type:
PROTEIN
Mol. Mass.:
64559.49
Organism:
Homo sapiens (Human)
Description:
ChEMBL_586859
Residue:
567
Sequence:
MGRGLLRGLWPLHIVLWTRIASTIPPHVQKSVNNDMIVTDNNGAVKFPQLCKFCDVRFSTCDNQKSCMSNCSITSICEKPQEVCVAVWRKNDENITLETVCHDPKLPYHDFILEDAASPKCIMKEKKKPGETFFMCSCSSDECNDNIIFSEEYNTSNPDLLLVIFQVTGISLLPPLGVAISVIIIFYCYRVNRQQKLSSTWETGKTRKLMEFSEHCAIILEDDRSDISSTCANNINHNTELLPIELDTLVGKGRFAEVYKAKLKQNTSEQFETVAVKIFPYEEYASWKTEKDIFSDINLKHENILQFLTAEERKTELGKQYWLITAFHAKGNLQEYLTRHVISWEDLRKLGSSLARGIAHLHSDHTPCGRPKMPIVHRDLKSSNILVKNDLTCCLCDFGLSLRLDPTLSVDDLANSGQVGTARYMAPEVLESRMNLENVESFKQTDVYSMALVLWEMTSRCNAVGEVKDYEPPFGSKVREHPCVESMKDNVLRDRGRPEIPSFWLNHQGIQMVCETLTECWDHDPEARLTAQCVAERFSELEHLDRLSGRSCSEEKIPEDGSLNTTK
  
Inhibitor
Name:
BDBM50468191
Synonyms:
CHEMBL4279160
Type:
Small organic molecule
Emp. Form.:
C20H17N5O2
Mol. Mass.:
359.3813
SMILES:
COc1ccc(cn1)-c1c([nH]c2cccnc12)-c1ccnc(NC(C)=O)c1
Structure:
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