Target
Activin receptor type-1 [R206H]
Ligand
BDBM488080
Substrate
n/a
Meas. Tech.
Enzyme Inhibitory Assay
IC50
2.70±n/a nM
Citation
 Hashizume, YSekimata, KKubota, HYamamoto, HKoda, YKoyama, HTaguri, TSato, TTanaka, AMiyazono, K BMP-signal-inhibiting compound US Patent  US10954216 Publication Date 3/23/2021 
Target
Name:
Activin receptor type-1 [R206H]
Synonyms:
ACVR1 | ACVR1_HUMAN | ACVRLK2 | Activin receptor type-1 (ALK-2)(R206H)
Type:
Enzyme Catalytic Domain
Mol. Mass.:
57138.77
Organism:
Homo sapiens (Human)
Description:
Q04771[R206H]
Residue:
509
Sequence:
MVDGVMILPVLIMIALPSPSMEDEKPKVNPKLYMCVCEGLSCGNEDHCEGQQCFSSLSINDGFHVYQKGCFQVYEQGKMTCKTPPSPGQAVECCQGDWCNRNITAQLPTKGKSFPGTQNFHLEVGLIILSVVFAVCLLACLLGVALRKFKRRNQERLNPRDVEYGTIEGLITTNVGDSTLADLLDHSCTSGSGSGLPFLVQRTVAHQITLLECVGKGRYGEVWRGSWQGENVAVKIFSSRDEKSWFRETELYNTVMLRHENILGFIASDMTSRHSSTQLWLITHYHEMGSLYDYLQLTTLDTVSCLRIVLSIASGLAHLHIEIFGTQGKPAIAHRDLKSKNILVKKNGQCCIADLGLAVMHSQSTNQLDVGNNPRVGTKRYMAPEVLDETIQVDCFDSYKRVDIWAFGLVLWEVARRMVSNGIVEDYKPPFYDVVPNDPSFEDMRKVVCVDQQRPNIPNRWFSDPTLTSLAKLMKECWYQNPSARLTALRIKKTLTKIDNSLDKLKTDC
  
Inhibitor
Name:
BDBM488080
Synonyms:
N-(4-(1-Ethyl-3- (pyridin-3-yl)-1H- pyrazol-4- yl)pyrimidin-2-yl)-2- methyl-1,2,3,4- tetrahydroisoquinolin- 6-amine | US10954216, Example 129
Type:
Small organic molecule
Emp. Form.:
C24H25N7
Mol. Mass.:
411.5022
SMILES:
CCn1cc(c(n1)-c1cccnc1)-c1ccnc(Nc2ccc3CN(C)CCc3c2)n1
Structure:
Search PDB for entries with ligand similarity: