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Target
TGF-beta receptor type-2
Ligand
BDBM282805
Substrate
n/a
Meas. Tech.
ChEMBL_1838892 (CHEMBL4339025)
IC50
>15000±n/a nM
Citation
 Velaparthi, U; Darne, CP; Warrier, J; Liu, P; Rahaman, H; Augustine-Rauch, K; Parrish, K; Yang, Z; Swanson, J; Brown, J; Dhar, G; Anandam, A; Holenarsipur, VK; Palanisamy, K; Wautlet, BS; Fereshteh, MP; Lippy, J; Tebben, AJ; Sheriff, S; Ruzanov, M; Yan, C; Gupta, A; Gupta, AK; Vetrichelvan, M; Mathur, A; Gelman, M; Singh, R; Kinsella, T; Murtaza, A; Fargnoli, J; Vite, G; Borzilleri, RM Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGF?R1 Inhibitor as an Immuno-oncology Agent. ACS Med Chem Lett 11:172-178 (2020) [PubMed]  Article 
Target
Name:
TGF-beta receptor type-2
Synonyms:
TGF-beta receptor type II | TGFBR2 | TGFR2_HUMAN
Type:
PROTEIN
Mol. Mass.:
64559.49
Organism:
Homo sapiens (Human)
Description:
ChEMBL_586859
Residue:
567
Sequence:
MGRGLLRGLWPLHIVLWTRIASTIPPHVQKSVNNDMIVTDNNGAVKFPQLCKFCDVRFSTCDNQKSCMSNCSITSICEKPQEVCVAVWRKNDENITLETVCHDPKLPYHDFILEDAASPKCIMKEKKKPGETFFMCSCSSDECNDNIIFSEEYNTSNPDLLLVIFQVTGISLLPPLGVAISVIIIFYCYRVNRQQKLSSTWETGKTRKLMEFSEHCAIILEDDRSDISSTCANNINHNTELLPIELDTLVGKGRFAEVYKAKLKQNTSEQFETVAVKIFPYEEYASWKTEKDIFSDINLKHENILQFLTAEERKTELGKQYWLITAFHAKGNLQEYLTRHVISWEDLRKLGSSLARGIAHLHSDHTPCGRPKMPIVHRDLKSSNILVKNDLTCCLCDFGLSLRLDPTLSVDDLANSGQVGTARYMAPEVLESRMNLENVESFKQTDVYSMALVLWEMTSRCNAVGEVKDYEPPFGSKVREHPCVESMKDNVLRDRGRPEIPSFWLNHQGIQMVCETLTECWDHDPEARLTAQCVAERFSELEHLDRLSGRSCSEEKIPEDGSLNTTK
  
Inhibitor
Name:
BDBM282805
Synonyms:
6-(4-(4-fluorophenyl)-1-(2-hydroxyethyl)-1H-imidazol- 5-yl)imidazo[1,2-b]pyridazine-3-carbonitrile | US10287295, Example 14' | US11352360, Example 14' | US9884868, Example 14'
Type:
Small organic molecule
Emp. Form.:
C18H13FN6O
Mol. Mass.:
348.3338
SMILES:
OCCn1cnc(c1-c1ccc2ncc(C#N)n2n1)-c1ccc(F)cc1
Structure:
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