Reaction Details Report a problem with these data
Target
TGF-beta receptor type-1
Ligand
BDBM645457
Substrate
n/a
Meas. Tech.
In vitro Assay
IC50
<1.000±n/a nM
Citation
 PIZZIRANI, D; BIAGETTI, M; RONCHI, P; BRUNO, P; GUARIENTO, S; BERTANI, B; PALA, D; BARILLI, A PYRIDAZINYL AMINO DERIVATIVES AS ALK5 INHIBITORS US Patent  US20240018122 Publication Date 1/18/2024 
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:
BDBM645457
Synonyms:
US20240018122, Example 129 | oxetan-3-yl 4-{2-[(4-{[6-(5- chloro-2-fluorophenyl)-3- methylpyridazin-4- yl]amino}pyridin-2- yl)carbamoyl]ethyl}-1- methylpiperazine-2- carboxylate
Type:
Small organic molecule
Emp. Form.:
C28H31ClFN7O4
Mol. Mass.:
584.042
SMILES:
CN1CCN(CCC(=O)Nc2cc(Nc3cc(nnc3C)-c3cc(Cl)ccc3F)ccn2)CC1C(=O)OC1COC1
Structure:
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