Target
TGF-beta receptor type-1
Ligand
BDBM481192
Substrate
n/a
Meas. Tech.
Kinase Activity Assay
IC50
34.0±n/a nM
Citation
 Yu, SYang, FYan, JWu, XHe, FTao, W Five-membered heteroaryl ring bridged ring derivative, preparation method therefor and medical use thereof US Patent  US10906905 Publication Date 2/2/2021 
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:
BDBM481192
Synonyms:
2-(6-Methylpyridin-2-yl)-3-(2-(4-(methylsulfonyl)phenyl)pyridin-4-yl)-4,5,6,7-tetrahydro-4,7-ethanopyrazolo[1,5-a]pyridine 33 | US10906905, Example 33
Type:
Small organic molecule
Emp. Form.:
C27H26N4O2S
Mol. Mass.:
470.586
SMILES:
Cc1cccc(n1)-c1nn2C3CCC(CC3)c2c1-c1ccnc(c1)-c1ccc(cc1)S(C)(=O)=O |(-3.04,-8.62,;-3.04,-7.08,;-4.37,-6.31,;-4.37,-4.77,;-3.04,-4,;-1.71,-4.77,;-1.71,-6.31,;-.37,-4,;1.2,-5.23,;2.06,-3.48,;3.6,-3.48,;4.37,-2.14,;3.6,-.81,;2.06,-.81,;3.01,-1.14,;3.78,-2.47,;1.29,-2.14,;-.21,-2.46,;-1.36,-1.43,;-2.82,-1.91,;-3.97,-.88,;-3.65,.63,;-2.18,1.1,;-1.04,.07,;-1.86,2.61,;-.4,3.09,;-.08,4.59,;-1.22,5.62,;-2.69,5.15,;-3.01,3.64,;-.9,7.13,;-.57,8.62,;.59,6.73,;-2.39,7.53,)|
Structure:
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