| Reaction Details |
|---|
 | Report a problem with these data |
| Target | TGF-beta receptor type-1 |
|---|
| Ligand | BDBM2579 |
|---|
| Substrate/Competitor | n/a |
|---|
| Meas. Tech. | ChEMBL_1349288 (CHEMBL3268788) |
|---|
| IC50 | >18500±n/a nM |
|---|
| Citation |  Jin, CH; Krishnaiah, M; Sreenu, D; Subrahmanyam, VB; Rao, KS; Lee, HJ; Park, SJ; Park, HJ; Lee, K; Sheen, YY; Kim, DK Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-ß type I receptor kinase as cancer immunotherapeutic/antifibrotic agent. J Med Chem57:4213-38 (2014) [PubMed] Article |
|---|
| More Info.: | Get all data from this article, Assay Method |
|---|
| |
| TGF-beta receptor type-1 |
|---|
| 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: | MEAAVAAPRPRLLLLVLAAAAAAAAALLPGATALQCFCHLCTKDNFTCVTDGLCFVSVTE
TTDKVIHNSMCIAEIDLIPRDRPFVCAPSSKTGSVTTTYCCNQDHCNKIELPTTVKSSPG
LGPVELAAVIAGPVCFVCISLMLMVYICHNRTVIHHRVPNEEDPSLDRPFISEGTTLKDL
IYDMTTSGSGSGLPLLVQRTIARTIVLQESIGKGRFGEVWRGKWRGEEVAVKIFSSREER
SWFREAEIYQTVMLRHENILGFIAADNKDNGTWTQLWLVSDYHEHGSLFDYLNRYTVTVE
GMIKLALSTASGLAHLHMEIVGTQGKPAIAHRDLKSKNILVKKNGTCCIADLGLAVRHDS
ATDTIDIAPNHRVGTKRYMAPEVLDDSINMKHFESFKRADIYAMGLVFWEIARRCSIGGI
HEDYQLPYYDLVPSDPSVEEMRKVVCEQKLRPNIPNRWQSCEALRVMAKIMRECWYANGA
ARLTALRIKKTLSQLSQQEGIKM
|
|
|
|---|
| BDBM2579 |
|---|
| n/a |
|---|
| Name | BDBM2579 |
|---|
| Synonyms: | (2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one | CHEMBL388978 | Staurosporin, 4 | Staurosporine | Staurosporine, 8 | US20240002365, Compound staurosporine | US9206188, Staurosporine | US9226923, Staurosporine |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C28H26N4O3 |
|---|
| Mol. Mass. | 466.531 |
|---|
| SMILES | CN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r| |
|---|
| Structure | 
|
|---|
Search and Browse
