Reaction Details Report a problem with these data
Target
TGF-beta receptor type-1
Ligand
BDBM645501
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:
BDBM645501
Synonyms:
US20240018122, Example 187 | methyl 3-[6-(5-chloro-2- fluorophenyl)-4-({2-[3-(4- methylpiperazin-1- yl)propanamido]pyridin-4- yl}amino)pyridazin-3- yl]propanoate
Type:
Small organic molecule
Emp. Form.:
C27H31ClFN7O3
Mol. Mass.:
556.032
SMILES:
COC(=O)CCc1nnc(cc1Nc1ccnc(NC(=O)CCN2CCN(C)CC2)c1)-c1cc(Cl)ccc1F
Structure:
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