Reaction Details Report a problem with these data
Target
TGF-beta receptor type-1
Ligand
BDBM280340
Substrate
n/a
Meas. Tech.
In Vitro Kinase Assay - Inhibition of ALK1/2/3/4/5/6 Kinases
IC50
15.7±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:
BDBM280340
Synonyms:
(S)-4-(2-(5-chloro-2-fluorophenyl)-5-isopropylpyridin-4-ylamino)-N-(1-hydroxypropan-2-yl)nicotinamide | US10030004, Compound 6a | US10501436, Compound 6a | US11053216, Compound 6a | US11702401, Compound 6a
Type:
Small organic molecule
Emp. Form.:
C23H24ClFN4O2
Mol. Mass.:
442.914
SMILES:
CC(C)c1cnc(cc1Nc1ccncc1C(=O)N[C@@H](C)CO)-c1cc(Cl)ccc1F |r|
Structure:
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