Target
Activin receptor type-1 [R206H]
Ligand
BDBM488036
Substrate
n/a
Meas. Tech.
Enzyme Inhibitory Assay
IC50
15.1±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:
BDBM488036
Synonyms:
N-(4-(1-Ethyl-1H- pyrazol-4-yl)phenyl)- 4-(1-ethyl-3-(pyridin- 3-yl)-1H-pyrazol-4- yl)pyrimidin-2-amine | US10954216, Example 27
Type:
Small organic molecule
Emp. Form.:
C25H24N8
Mol. Mass.:
436.5117
SMILES:
CCn1cc(cn1)-c1ccc(Nc2nccc(n2)-c2cn(CC)nc2-c2cccnc2)cc1
Structure:
Search PDB for entries with ligand similarity: