Target
TGF-beta receptor type-1
Ligand
BDBM481199
Substrate
n/a
Meas. Tech.
Kinase Activity Assay
IC50
9.00±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:
BDBM481199
Synonyms:
3-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-2-(6-methylpyridin-2-yl)-4,5,6,7-tetrahydro-4,7-ethanopyrazolo[1,5-a]pyridine 38 | US10906905, Example 38
Type:
Small organic molecule
Emp. Form.:
C21H20N6
Mol. Mass.:
356.4237
SMILES:
Cc1cccc(n1)-c1nn2C3CCC(CC3)c2c1-c1ccc2ncnn2c1 |TLB:8:9:11.12:15.14,THB:17:16:11.12:15.14,(-2.95,-5.87,;-2.95,-4.33,;-4.29,-3.56,;-4.29,-2.02,;-2.95,-1.25,;-1.62,-2.02,;-1.62,-3.56,;-.28,-1.25,;1.43,-2.25,;2.15,-.73,;3.69,-.73,;4.46,.6,;3.69,1.94,;2.15,1.94,;3.13,1.63,;3.9,.3,;1.38,.6,;-.12,.28,;-1.27,1.31,;-2.73,.84,;-3.88,1.87,;-3.56,3.38,;-4.46,4.62,;-3.56,5.87,;-2.09,5.39,;-2.09,3.85,;-.95,2.82,)|
Structure:
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