Reaction Details Report a problem with these data
Target
TGF-beta receptor type-1
Ligand
BDBM280356
Substrate
n/a
Meas. Tech.
In Vitro Kinase Assay - Inhibition of ALK1/2/3/4/5/6 Kinases
IC50
16.9±n/a nM
Citation
 Rai, R; Chakravarty, S; Pujala, B; Shinde, BU; Nayak, AK; Agarwal, AK; Ramachandran, SA; Pham, SM Compounds and methods of use US Patent  US11702401 Publication Date 7/18/2023 
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:
BDBM280356
Synonyms:
4-[[2-amino-6-(5-chloro-2-fluoro-phenyl)-3-isopropenyl-4-pyridyl]amino]-N-[(2S)-2-hydroxypropyl]pyridine-3-carboxamide | US10030004, Compound 23a | US11053216, Compound 23a | US11702401, Compound 23a
Type:
Small organic molecule
Emp. Form.:
C26H26ClFN4O4
Mol. Mass.:
512.96
SMILES:
COC(=O)c1cnccc1Nc1cc(nc(NC(=O)OC(C)(C)C)c1C(C)=C)-c1cc(Cl)ccc1F
Structure:
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