Target
TGF-beta receptor type-1
Ligand
BDBM412745
Substrate
n/a
Meas. Tech.
ChEMBL_1753651 (CHEMBL4188411)
Ki
0.220000±n/a nM
Citation
 Harikrishnan, LSWarrier, JTebben, AJTonukunuru, GMadduri, SRBaligar, VMannoori, RSeshadri, BRahaman, HArunachalam, PNDikundwar, AGFink, BEFargnoli, JFereshteh, MFan, YLippy, JHo, CPWautlet, BSheriff, SRuzanov, MBorzilleri, RM Heterobicyclic inhibitors of transforming growth factor beta receptor I (TGF?RI). Bioorg Med Chem 26:1026-1034 (2018) [PubMed]  Article 
Target
Name:
TGF-beta receptor type-1
Synonyms:
ALK-5 | ALK5 | Activin A receptor type II-like protein kinase of 53kD | Activin receptor-like kinase 5 | SKR4 | Serine/threonine-protein kinase receptor R4 | TGF-beta receptor type I | TGF-beta type I receptor | TGFBR1 | TGFR-1 | TGFR1_HUMAN | TbetaR-I | Transforming growth factor-beta receptor type I
Type:
enzyme
Mol. Mass.:
55968.24
Organism:
Homo sapiens (Human)
Description:
P36897
Residue:
503
Sequence:
MEAAVAAPRPRLLLLVLAAAAAAAAALLPGATALQCFCHLCTKDNFTCVTDGLCFVSVTETTDKVIHNSMCIAEIDLIPRDRPFVCAPSSKTGSVTTTYCCNQDHCNKIELPTTVKSSPGLGPVELAAVIAGPVCFVCISLMLMVYICHNRTVIHHRVPNEEDPSLDRPFISEGTTLKDLIYDMTTSGSGSGLPLLVQRTIARTIVLQESIGKGRFGEVWRGKWRGEEVAVKIFSSREERSWFREAEIYQTVMLRHENILGFIAADNKDNGTWTQLWLVSDYHEHGSLFDYLNRYTVTVEGMIKLALSTASGLAHLHMEIVGTQGKPAIAHRDLKSKNILVKKNGTCCIADLGLAVRHDSATDTIDIAPNHRVGTKRYMAPEVLDDSINMKHFESFKRADIYAMGLVFWEIARRCSIGGIHEDYQLPYYDLVPSDPSVEEMRKVVCEQKLRPNIPNRWQSCEALRVMAKIMRECWYANGAARLTALRIKKTLSQLSQQEGIKM
  
Inhibitor
Name:
BDBM412745
Synonyms:
N-(3-fluoropyridin-4-yl)-2-(6-(trifluoromethyl)pyridin-2-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine | US10399987, Example 10
Type:
Small organic molecule
Emp. Form.:
C17H10F4N6
Mol. Mass.:
374.2951
SMILES:
Fc1cnccc1Nc1nc(nc2[nH]ccc12)-c1cccc(n1)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity: